T0078 |
LapatinibHOT |
Lapatinib is a dual inhibitor of Lapatinib is a dual ErbB2/EGFR (IC50: 9.2/10.8 nM) inhibitor |
T0078L |
Lapatinib ditosylate monohydrate |
Lapatinib is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib therapy is associated with tra...
|
T0129 |
Sanguinarine chloride |
Sanguinarine chloride, a benzophenanthridine alkaloid, stimulates apoptosis by activating the production of reactive oxygen species (ROS). |
T0373 |
ErlotinibHOT |
Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer. |
T0373L |
Erlotinib hydrochlorideHOT |
Erlotinib is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer. |
T0801 |
Tannic acid |
Tannic acid is a novel hERG channel blocker. |
T10256 |
Afatinib D6 |
Afatinib D6 (BIBW 2992 D6) is a deuterium-labeled Afatinib. Afatinib is an irreversible EGFR family inhibitor. |
T10419 |
AV-412 |
AV-412 is an EGFR inhibitor (EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M and ErbB2 with IC50s of 0.75, 0.79, 0.5, 2.3, 19 nM). |
T10433 |
Osimertinib dimesylate |
Osimertinib dimesylate is an irreversible and mutant selective EGFR inhibitor (IC50s: 12 and 1 nM against EGFR L858R and EGFR L858R/T790M). |
T10531 |
BGB-102 |
BGB-102 is a potent multi-kinase inhibitor against HER2, EGFR, and HER4 (IC50s: 18 nM, 9.6 nM, and 40.3 nM). |
T10534 |
BI-4020 |
BI-4020 is a fourth-generation, non-covalent, and orally active inhibitor of EGFR tyrosine kinase. |
T10556 |
BKI-1369 |
BKI-1369 is a bumped kinase inhibitor. BKI-1369 increases hERG-inhibitory activity (IC50:1.52 μM). |
T10802 |
CHMFL-EGFR-202 |
CHMFL-EGFR-202 is a potent, irreversible inhibitor of EGFR mutant kinase (IC50s: 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases). |
T10965 |
DBPR112 |
DBPR112 has an IC50 of 15 nM and 48 nM for EGFRWT and EGFRL858R / T790M, respectively. It is an oral active epidermal growth factor receptor inhibitor based on ...
|
T11157 |
EGFR-IN-1 |
EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity. EGFR-IN-1 is an orall...
|
T11157L |
EGFR-IN-1 hydrochloride |
EGFR-IN-1 hydrochloride displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity. EGFR-IN...
|
T11158 |
EGFR-IN-11 |
EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.EGFR-IN-11 is a fourth-generation EGFR-tyrosi...
|
T11159 |
EGFR-IN-2 |
EGFR-IN-2 is a non-covalent, mutation-selective and irreversible second-generation EGFR inhibitor. |
T11160 |
EGFR-IN-5 |
EGFR-IN-5 is a EGFR inhibitor, EGFR-IN-5 with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFRL858R, EGFRL858R/T790M, and EGFRL858R/T790M/C797S, respectively. |
T11161 |
EGFR-IN-7 |
EGFR-IN-7 is a selective and potent EGFR kinase inhibitor. |
T11162 |
EGFR-IN-8 |
EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC. EGFR-IN-8 is a dual EGFR and c-Met inhibitor. |
T11163 |
EGFR-IN-9 |
EGFR-IN-9 has antitumor activity. EGFR-IN-9 is a potent EGFR kinase inhibitor with IC50s of 7 nM, 28 nM for the wild type EGFR kinase and double mutant EGFR kin...
|
T11164 |
EGFR mutant-IN-1 |
EGFR mutant- in-1, A 5-methylpyrimidopyridone derivative are effective selective EGFRL858R/T790M/C797S mutant inhibitors with IC50 of 27.5 nM, which significant...
|
T11213 |
Epertinib hydrochloride |
Epertinib hydrochloride shows potent antitumor activity. Epertinib hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibito...
|
T11213L |
Epertinib |
Epertinib is a reversible and selective tyrosine kinase inhibitor of EGFR, HER2, and HER4 (IC50s: 1.48 nM, 7.15 nM, and 2.49 nM). It displays a strong antitumor...
|
T1144L |
Lidocaine Hydrochloride hydrate |
Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property. |
T11569 |
HKI-357 |
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 (IC50s: 34 nM and 33 nM). HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK p...
|
T11717 |
JHU395 |
JHU395 delivers 6-diazo-5-oxo-L-norleucine (DON) to malignant peripheral nerve sheath tumor (MPNST) in vitro and in vivo, and has antitumor activity in MPNST. J...
|
T1181 |
GefitinibHOT |
Gefitinib is an EGFR tyrosine kinase inhibitor and can inhibit Tyr1173, Tyr992, Tyr1173 and Tyr992 (IC50s: 37/37/26/57 nM). |
T12130 |
Mutated EGFR-IN-2 |
Mutated EGFR-IN-2 is an inhibitor of mutant-selective EGFR. |
T12131 |
Mutated EGFR-IN-3 |
Mutated EGFR-IN-3 is a ATP-competitive and highly selective allosteric dibenzodiazepinone EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) inhibitor(IC50 of 12 nM ...
|
T12175 |
Naquotinib mesylate |
Naquotinib mesylate is an orally available, mutant-selective and irreversible inhibitor of EGFR(iC50s of 8-33 nM and 230 nM for toward EGFR mutants and EGFR). |
T1266 |
Terfenadine |
Terfenadine is a prodrug that is metabolized by intestinal CYP3A4 to the active form fexofenadine, a selective histamine H1-receptor antagonist with antihistami...
|
T12777 |
RTC-5 |
RTC-5 demonstrated efficacy against a xenograft model of an EGFR driven cancer without the neurotropic effects exhibited by the parent molecules. Its effects we...
|
T1291 |
Cisapride |
Cisapride is a serotonin type 4 (5-HT4) receptor agonists are potent prokinetic agents that act on serotonin receptors in the intestine and promote intestinal p...
|
T12912 |
Sigma-1 receptor antagonist 3 |
Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain. |
T13088 |
Tarloxotinib bromide |
Tarloxotinib bromide is an irreversible inhibitor of EGFR/HER2. |
T13559 |
Astragaloside VI |
Astragaloside VI could improve wound healing by activating the EGFR/ERK signaling pathway. |
T13743 |
JH-XI-10-02 |
JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19. JH-XI-10-02 is a potent and selective degrad...
|
T14138 |
AG-825 |
AG-825(Tyrphostin AG-825) is a potential agent for overcoming Mn-induced neurotoxicity or AD development[5] and is a selective and ATP-competitive ErbB2 inhibit...
|
T14336 |
Allitinib |
Allitinib (AST-1306) is an orally active and irreversible EGFR and ErbB2 inhibitor with IC50s of 0.5 and 3 nM, respectively. Allitinib is an anilino-quinazoline...
|
T16362 |
Nuvenzepine |
Nuvenzepine is an antagonist of mAChR. It has the potential for gastrospasm treatment. |
T16369 |
O-Desmethyl gefitinib |
O-Desmethyl gefitinib inhibits EGFR (IC50: 36 nM in subcellular assays). In human plasma, O-Desmethyl gefitinib is an active metabolite of Gefitinib. The format...
|
T16492 |
PF-06459988 |
PF-06459988 is an irreversible T790M-Containing EGFR Mutants inhibitor. |
T1656 |
VandetanibHOT |
Vandetanib is a potent inhibitor of VEGFR2 (IC50: 40 nM). It also inhibits VEGFR3 and EGFR. |
T16996 |
TAS6417 |
TAS6417 is an EGFR inhibitor and is an efficacious drug candidate for patients with NSCLC (IC50: ranging from 1.1-8.0 nM). |
T1737 |
Genistein |
Genistein is an isoflavonoid derived from soy products. It inhibits protein-tyrosine kinase and topoisomerase-II (DNA TOPOISOMERASES, TYPE II), with antineoplas...
|
T1761 |
PD153035 hydrochloride |
PD153035 hydrochloride (ZM 252868; AG 1517) is a effective and selective inhibitor of EGFR (Ki: 5.2 pM, IC50: 29 pM); few influence against FGFR, PGDFR, InsR, C...
|
T1773 |
Afatinib Dimaleate |
Afatinib is an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EG...
|
T19489 |
O-Desmethyl gefitinib D8 |
O-Desmethyl gefitinib D8 is a deuterium labeled O-Desmethyl gefitinib that is an active metabolite of Gefitinib in human plasma. |
T19814 |
CP-380736 |
CP-380736 is an epidermal growth factor receptor (EGFR) inhibitor. EGFR is a tyrosine kinase that activates MAPK, JNK, and Akt pathways, and is an important med...
|
T1985 |
WHI-P154 |
WHI-P154 is a potent JAK3 inhibitor. |
T2032 |
WHI-P180 |
WHI-P180 is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively. |
T2034 |
AG1557 |
AG-1557 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194). |
T2035 |
WHI-P258 |
WHI-P258 is a dimethoxyquinazoline inhibitor of JAK3. This compound binds JAK3 weakly and may be used as a JAK-binding negative control in the development of ne...
|
T2041 |
PD153035 |
PD153035 hydrochloride is an effective and selective inhibitor of EGFR (Ki/IC50: 5.2/29 pM, in cell-free assays); little inhibitory against FGFR, PGDFR, InsR, C...
|
T2047 |
AG1478 |
AG-1478 (Tyrphostin AG-1478) is a selective EGFR inhibitor. |
T2055 |
WS3 |
WS3, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
T2063 |
AG18 |
AG-18 inhibits EGFR with IC50 of 35 μM. |
T2106 |
WS6 |
WS6, a β cell proliferation inducer, regulates Erb3 binding protein-1 (EBP1) and the IκB kinase pathway. |
T2116 |
AEE788 |
AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors. |
T21312 |
Afatinib free base |
Afatinib is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectivel...
|
T22272 |
Lifirafenib |
Lifirafenib (BGB-283) is a potent inhibitor of RAF family kinases and EGFR in biochemical assays with IC50 of 23, 29 and 495 nM for the recombinant BRAFV600E ki...
|
T22296 |
Cisapride hydrate |
Cisapride acts directly as a selective agonist of serotonin 5-HT4 receptor with IC50 value of 0.483 μM. And It also acts indirectly as a parasympathomimetic. |
T2245 |
CL387785 |
CL-387785(EKI785; WAY-EKI 785) is an irreversible inhibitor of EGFR(IC50: 370+/-120 pM); is able to overcome resistance caused by the T790M mutation on a ...
|
T2280 |
Endoxifen Z-isomer |
Endoxifen (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity. |
T2303 |
AfatinibHOT |
Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, res...
|
T2307 |
Icotinib Hydrochloride |
Icotinib Hydrochloride is the hydrochloride salt form of icotinib, an orally available quinazoline-based inhibitor of EGFR, with potential antineoplastic activi...
|
T2325 |
NeratinibHOT |
Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor for HER2 and EGFR (IC50: 59/92 nM), respectively. |
T2327 |
Pelitinib |
Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM). |
T2364 |
Irbinitinib |
Irbinitinib(ARRY-380; ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM). |
T2369 |
Rociletinib |
Rociletinib is an orally available small molecule, irreversible inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity. |
T2446 |
KI8751 |
KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM. |
T2460 |
JAK 3 inhibitor IV |
JAK 3 inhibitor IV is a JAK1/3 inhibitor with pIC50 of 4.4/7.1, almost no activity to JAK2 and modestly potent to EGFR; also found to be sensitive to transgluta...
|
T2479 |
Tyrphostin 9 |
Tyrphostin 9 is an Agricultural acaricide, now superseded. Tyrphostin 9 is firstly designed as an EGFR inhibitor |
T2483 |
Dacomitinib |
Dacomitinib(PF299804; PF-00299804) is a highly selective, orally bioavailable small-molecule inhibitor of the HER family of tyrosine kinases with IC50 of 6, 45....
|
T2490 |
Osimertinib |
Osimertinib is a small molecule tyrosine kinase receptor inhibitor and antineoplastic agent that is used in the therapy of selected forms of advanced non-small ...
|
T2491 |
AZ5104 |
AZ5104 is a potent EGFR inhibitor. |
T2501 |
Canertinib dihydrochloride |
Canertinib dihydrochloride is the hydrochloride salt of an orally bio-available quinazoline with potential antineoplastic and radiosensitizing activities. |
T2600 |
AG490 |
AG-490 (Tyrphostin AG 490) is an inhibitor of EGFR (IC50: 0.1 μM). It is 135-fold more selective for EGFR than ErbB2, also inhibits JAK2 with no effect to Lyn,...
|
T2642 |
PD173074 |
PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for...
|
T2705 |
Mutant EGFR inhibitor |
Mutant EGFR inhibitor is a selective and potent Mutated EGFR inhibitor, inhibits L858R activating mutant, the Exonl9 deletion activating mutant and the T790M re...
|
T2851 |
Daphnetin |
Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor with inhibitory for EGFR (IC50: 7.67 μM), PKA (IC50: 9.33 μM), and PKC (IC50: 25.01 μ...
|
T2859 |
Biochanin A |
Biochanin A is an isoflavone derivative isolated from red clover Trifolium pratense with anticarcinogenic properties. Biochanin A is a naturally occurring fatty...
|
T2894 |
Norcantharidin |
Norcantharidin is a synthetic anticancer compound which is a dual inhibitor for c-Met and EGFR in human colon cancers. |
T2959 |
Ginsenoside Rh2 |
Ginsenoside Rh2, an extract of red Panax ginseng, is a potent anti-inflammatory and anticancer drug. |
T2995 |
Chrysophanic Acid |
Chrysophanic acid is an EGFR/mTOR pathway inhibitor, which can be found in rhubarb, and sorrel. |
T2S0961 |
Chalcone |
Chalcone is an aromatic ketone that forms the central core for a variety of important biological compounds, which are known collectively as chalcones. |
T3024 |
Avitinib |
Avitinib, also known as AC0010 or AC0010MA, is an orally available, irreversible, epidermal growth factor receptor (EGFR) mutant-selective inhibitor, with poten...
|
T3059 |
AP26113 |
AP26113 is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. ...
|
T3108 |
CUDC101 |
CUDC-101 is a potent inhibitor of HDAC, EGFR and HER2 with IC50s of 4.4, 2.4 and 15.7 nM, respectively. |
T3192 |
NS1643 |
NS1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM. |
T3402 |
Ginsenoside Rg3 |
Ginsenoside Rg3 possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells. It inhibits the pro...
|
T3506 |
Nazartinib |
Nazartinib (EGF816, NVS-816) is a covalent, irreversible, mutant-selective EGFR inhibitor that has nanomolar inhibitory potency against activating mt (L858R, ex...
|
T3545 |
RG 13022 |
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor (IC50: 4 μM). |
T3554 |
RG 14620 |
RG14620 is an epidermal growth factor receptor (EGFR) inhibitor. |
T3558 |
EBE-A22 |
EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive. |
T3621 |
Brigatinib |
Brigatinib is a highly potent and selective ALK inhibitor. |
T3634 |
Osimertinib mesylateHOT |
Osimertinib (AZD-9291) is an irreversible and mutant selective EGFR inhibitor (IC50s: 12/1 nM for EGFR(L858R) and EGFR(L858R/T790M)). |
T3659 |
AZD3759 |
AZD3759 is an orally active, effective and central nervous system-penetrant EGFR inhibitor. The IC50 values were 0.2, 0.3 and 0.2 nM for EGFR L858R mutant, TK w...
|
T3721 |
Avitinib maleate |
Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor. |
T3851 |
Vicenin -2 |
Vicenin 2 is an angiotensin-converting enzyme (ACE) inhibitor (IC50=43.83 μM) from the aerial parts of Desmodium styracifolium. Vicenin 2 is an inhibitor of α...
|
T3870 |
Cyasterone |
Cyasterone, a natural EGFR inhibitor, can inhibit the growth of A549 and MGC823 cells, via regulating EGFR signaling pathway, it may be a promising anti-cancer ...
|
T3P2855 |
Chamigrenal |
β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7...
|
T4014 |
CP724714 |
CP-724714 is an effective and selective HER2/ErbB2 inhibitor (IC50: 10 nM), >640-fold selectivity against EGFR, Abl, InsR, PDGFR, IRG-1R, Src, VEGFR2, c-Met etc...
|
T4183 |
lavendustin A |
lavendustin A is a potent, cell-permeable inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase. |
T4185 |
lavendustin C |
Lavendustin C is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase. |
T4205 |
AG 494 |
AG-494 is an inhibitor of epidermal growth factor receptor kinase. |
T4249 |
AZD3759 hydrochloride |
AZD3759 (hydrochloride) is an effective, orally active and central nervous system-penetrant EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.2/0.3/...
|
T4296 |
MTX211 |
MTX-211, an inhibitor of EGFR and PI3K, is used for the therapy of cancer and other diseases. |
T4326 |
AG 555 |
AG 555 is an EGFR tyrosine kinase inhibitor. |
T4485 |
Lazertinib |
Lazertinib is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T...
|
T4528 |
Tyrphostin AG 528 |
Tyrphostin AG 528 is an inhibitor of EGFR (IC50: 4.9 μM) and ErbB2 (IC50: 2.1 μM). |
T4612 |
NS309 |
NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for S...
|
T4612 |
NS309 |
NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for S...
|
T4694 |
AG-1557 hydrochloride (189290-58-2(free base)) |
AG-1557 is an inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase (pIC50: 8.194). |
T5155 |
AG 99 |
AG-99 is an inhibitor of EGFR kinase (IC50: 10 µM in the human epidermoid carcinoma cell line A431). |
T5168 |
EGFR Inhibitor |
EGFR inhibitor is a cell permeable and selective inhibitor of EGFR kinase (IC50: 21 nM) and blocks receptor autophosphorylation in cells. |
T5410 |
PD158780 |
PD 158780 reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor superfamily: EGFR, ErbB2, ErbB3, and ErbB4 (IC50s: 8μM, 49...
|
T5437 |
Gefitinib-based PROTAC 3 |
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827...
|
T5462 |
HS-10296 |
Hs-10296 is an inhibitor of EGFR activation mutation and tolerant mutation of EGFR T790M, which has only limited activity against wild-type EGFR. |
T5475 |
ZD-4190 |
ZD-4190 is a inhibitor of the vascular endothelial cell growth factor receptor 2 (VEGFR2) and of epidermal growth factor receptor (EGFR) signalling, used for th...
|
T5675 |
HS-10296 hydrochloride |
HS-10296 hydrochloride is a small molecule inhibitor of EGFR-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR. |
T6008 |
CNX2006 |
CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. |
T6036 |
Brivanib |
Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3...
|
T6039 |
TAK285 |
TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aur...
|
T6078 |
SaracatinibHOT |
Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes. |
T6092 |
Sapitinib |
AZD8931, a reversible, ATP competitive inhibitor of EGFR(IC50=4 nM), ErbB2(IC50=3 nM) and ErbB3(IC50=4 nM), is more effective over Gefitinib or Lapatinib agains...
|
T6124 |
Mubritinib |
Mubritinib (TAK-165) is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM. |
T6136 |
Canertinib |
Canertinib is a pan-erbB tyrosine kinase inhibitor which work against esophageal squamous cell carcinoma in vitro and in vivo. Canertinib treatment significantl...
|
T6153 |
Icotinib |
Icotinib is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity. |
T6196 |
PP1 |
PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively. |
T6227 |
Benidipine hydrochloride |
Benidipine HCl, a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel. |
T6235 |
Lapatinib DitosylateHOT |
Lapatinib is an effective EGFR and ErbB2 inhibitor (IC50: 10.8/9.2 nM for EGFR/ErbB2). |
T6238 |
WZ4002 |
WZ4002 is a mutant-selective EGFR inhibitor for EGFR(L858R) and EGFR(T790M) with IC50 of 2 nM/8 nM. |
T6266 |
PP2 |
PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2. |
T6328 |
Desmethyl Erlotinib |
OSI-420 is the active metabolite of Erlotinib (EGFR inhibitor with IC50 of 2 nM). |
T6331 |
AST-1306 TsOH |
AST-1306 is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, respectively. |
T6427 |
Butein |
Butein, a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit ...
|
T6619 |
OSI420 |
OSI-420 (Desmethyl Erlotinib, CP-473420) is an active metabolite of erlotinib which is an orally active EGFR tyrosin kinase inhibitor with IC50 of 2 and 20 nM f...
|
T6712 |
Tyrphostin AG 879 |
Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR. |
T6733 |
WZ3146 |
WZ3146 is a mutant-selective irreversible inhibitor of EGFR(L858R) and EGFR(E746_A750) with IC50 of 2 nM and 2 nM; does not inhibit ERBB2 phosphorylation (T798I...
|
T6734 |
WZ8040 |
WZ8040 is a novel mutant-selective irreversible EGFRT790M inhibitor, does not inhibit ERBB2 phosphorylation (T798I). |
T6824 |
EAI045 |
EAI045, an allosteric inhibitor, targets towards drug-resistant EGFR mutants but avoids the wild-type receptor. |
T6918 |
Olmutinib |
Olmutinib is an orally available small molecule, a mutant-selective inhibitor of epidermal growth factor receptor (EGFR) with potential antineoplastic activity....
|
T6932 |
PD168393 |
PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin. |
T7175 |
AST2818 mesylate |
AST2818 mesylate,is an irreversible tyrosine kinase inhibitor that selectively inhibits EGFR mutations, especially T790M. |
T7198 |
E-4031 |
E-4031 is a methanesulfonanilide class III antiarrhythmic agent that prolongs cardiac action potential duration by blocking ERG K+ channels (IC50 = 29 nM) |
T7322 |
Theliatinib |
Theliatinib, a potent and highly selective EGFR inhibitor, with anti-tumor activity. Ki of 0.05 nM for wild type EGFR, and IC50s of 3 and 22 nM for EGFR and EGF...
|
T7649 |
Tyrphostin A1 |
Tyrphostin A1 is an inhibitor of EGFR tyrosine kinase . |
T8151 |
Mobocertinib |
Mobocertinib is a potent inhibitor of epidermal growth factor receptor (EGFR) and an antineoplastic agent |
T8189 |
Dihydroberberine |
Dihydroberberine has anti-atherosclerotic, anti-inflammatory, hypolipidemic and antitumor activities. It inhibits human ether-a-go-go-related gene (hERG) channe...
|
T8431 |
JCN037 |
JCN037 is potent, non-covalent and brain-penetrant inhibitor of EGFR(EGFR, p-wtEGFR and pEGFRvⅢ with IC50 of 2.49 nM, 3.95 nM, 4.48 nM , respectively). |
T8460 |
Olmutinib |
Olmutinib is a Novel Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor |
T8534 |
Tyrphostin AG 112 |
Tyrphostin AG 112 is an inhibitor of EGFR phosphorylation. |
T8679 |
Epidermal Growth Factor |
Epidermal Growth Factor binds to epidermal growth factor receptor (EGFR) and stimulates cell growth and proliferation. It is approved for the treatment of diab...
|
T8751 |
AZD8931 diFuMaric acid |
AZD8931 is a reversible and ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 (IC50 of 4 nM, 3 nM and 4 nM, respectively). |
T8751 |
AZD8931 diFuMaric acid |
AZD8931 is a reversible and ATP competitive inhibitor of EGFR, ErbB2 and ErbB3 (IC50 of 4 nM, 3 nM and 4 nM, respectively). |
T8758 |
Poziotinib hydrochloride |
Poziotinib hydrochloride irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells...
|
T8872 |
(Rac)-JBJ-04-125-02 |
JBJ-04-125-02 is effective as a single agent in both in vitro and in vivo models of EGFR-mutant lung cancer. |
T9905 |
Cetuximab (anti-EGFR) |
Cetuximab (anti-EGFR) is an inhibitor of epidermal growth factor receptor (EGFR). |
T9905 |
Cetuximab (anti-EGFR) |
Cetuximab anti-EGFR) a novel molecular-targeted agentis an inhibitor of EGFR monoclonal humanized antibody interacting with the extracellular binding site of EG...
|
T9922 |
Matuzumab |
Matuzumab is a humanized monoclonal antibody used in cancer treatment. It has a high affinity for EGFR frequently associated with the growth of blood vessels in...
|
T9923 |
Nimotuzumab |
Nimotuzumab is a humanized therapeutic monoclonal antibody against epidermal growth factor receptor EGFR). |
T9927 |
Panitumumab |
Panitumumab is a fully human IgG2 monoclonal antibody targeting the epidermal growth factor receptor EGFR). |
TL0016 |
Sulforaphene |
Sulforaphene may be a potential anti- triple negative breast cancer natural compound and its /\''antiproliferation effects may be mediated by tumor suppressor E...
|
TMA1944 |
Protopine hydrochloride |
Protopine has antiplatelet effects,which is due to inhibition on thromboxane formation and phosphoinositides breakdown and then lead to the decrease of intracel...
|
TN1410 |
Asperulosidic acid |
Asperulosidic acid has been recently used in chinese medicine as a useful drug against some tumors. |
TN1871 |
Ligustroside |
Ligustroside shows little antioxidant, and anti-inflammatory properties, it shows a significant inhibition effect on prostaglandin E2 (PGE2)-release. Ligustrosi...
|
TN1912 |
Marinobufagenin |
Marinobufagenin, a cardiotonic steroid, its increased concentrations are important in the cardiac disease and oxidant stress state seen with renal failure. |
TN2309 |
Withanolide A |
Withanolide A extends the lifespan in human EGFR-driven cancerous Caenorhabditis elegans. |
TN2504 |
1,5-Dihydroxyxanthone |
1,5-Dihydroxyxanthone exhibits the epidermal growth factor receptor (EGFR) -tyrosine kinase inhibitory activity, with the IC50 value of 90.34 nM. It may have an...
|
TN3042 |
4-Hydroxycinnamamide |
4-Hydroxycinnamamide has antioxidant activity. 4-Hydroxycinnamamide derivatives are specific inhibitors of tyrosine-specific protein kinases. |
TN3525 |
Boehmenan |
(±)-Boehmenan shows potent protein-tyrosine phosphatase 1B (PTP1B) inhibitory activity in vitro with the IC(50) values of 43.5 uM, it inhibits PTP1B activity i...
|
TN3711 |
Corylifol C |
Corylifol C and, to a lesser extent, xanthoangelol are potent protein kinase inhibitors (inhibitory concentration 50% values for epidermal growth factor recepto...
|
TN4213 |
Hirsutenone |
Hirsutenone has potent antioxidant activity, it shows significant free radical scavenging activity and exhibits inhibition effect on the mitochondrial lipid per...
|
TN4638 |
Neolinine |
Neolinine(at 10uM) shows significant hERG K+ channel inhibition activity. |
TN5100 |
Taspine |
Taspine shows antitumor activity by modulating the EGFR signaling pathway of Erk1/2 and Akt in vitro and in vivo, it can inhibit growth and induce apoptosis of ...
|
TQ0092 |
Naquotinib |
Naquotinib (ASP8273) is an orally available, mutant-selective and irreversible EGFR inhibitor; (IC50s: 8-33 nM and 230 nM toward EGFR mutants and EGFR. |
TQ0166 |
Tesevatinib |
Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4)...
|
TQ0255 |
CK-101 |
CK-101 (RX-518) is a novel mutant-selective, irreversible, orally available EGFR inhibitor. It can overcome T790M-mediated resistance in NSCLC. |
TQ0271 |
Falnidamol |
Falnidamol (BIBX 1382) is a selective and orally active inhibitor of EGFR tyrosine kinase (IC50: 3 nM). |
TQ0293 |
AV-412 free base |
AV-412 free base is an EGFR inhibitor (IC50s: 0.75, 0.79, 0.5, 2.3, 19 nM for EGFR, EGFR(T790M), EGFR(L858R), EGFR(L858R/T790M) and ErbB2). |