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Angiogenesis Filter
Angiogenesis Tyrosine Kinase/AdaptorsACK1
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Src
Src kinase family is a family of non-receptor tyrosine kinases that includes nine members: Src, Yes, Fyn, and Fgr, forming the SrcA subfamily, Lck, Hck, Blk, and Lyn in the SrcB subfamily, and Frk in its own subfamily. Frk has homologs in invertebrates such as flies and worms, and Src homologs exist in organisms as diverse as unicellular choanoflagellates, but the SrcA and SrcB subfamilies are specific to vertebrates. Src family kinases contain six conserved domains: a N-terminal myristoylated segment, a SH2 domain, a SH3 domain, a linker region, a tyrosine kinase domain, and C-terminal tail.
Staurosporine
Cited
T668062996-74-1
Staurosporine (AM-2282) is a protein kinase inhibitor with ATP-competitive and non-selective inhibitory activity (IC50=6 15 2 3 3000 nM) against PKC, PKA, c-Fgr, phosphorylase kinase and TAOK2. Staurosporine also induces apoptosis.
- $56
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CitedSaracatinib Cited
T6078379231-04-6
Saracatinib (AZD0530) (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes.
- $59
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CitedeCF506
T84991914078-41-3
eCF506 is a potent and selective inhibitor of SRC (IC50 < 0.5 nM)
- $40
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Ibrutinib Cited
T1835936563-96-1
Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
- $36
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CitedNintedanib Cited
T1777656247-17-5
Nintedanib (Intedanib) is a triple vascular kinase inhibitor that inhibits VEGFR1, VEGFR2, and VEGFR3 (IC50=34 13 13 nM), FGFR1, FGFR2, and FGFR3 (IC50=69 37 108 nM), PDGFRα, and PDGFRβ (IC50=59 65 nM). Nintedanib has antitumor activity and inhibits tumor growth by inhibiting angiogenesis.
- $38
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CitedTofacitinib Cited
T6321477600-75-2
Tofacitinib (Tasocitinib) is a Janus kinase inhibitor that inhibits JAK3 2 1 (IC50=1 20 112 nM) and is orally active. Tofacitinib is used for the treatment of moderate to severe rheumatoid arthritis.
- $30
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CitedVemurafenib Cited
T2382918504-65-1
Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31 48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.
- $50
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CitedDasatinib Cited
T1448302962-49-8
Dasatinib (BMS-354825) is an orally active, ATP-competitive tyrosine kinase inhibitor that targets Src and Bcr-Abl (Ki=16 30 pM), with antitumor activity, used in the treatment of leukemia and lymphoma.
- $37
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CitedPonatinib Cited
T2372943319-70-8
Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor with IC50 values of 0.37 nM (Abl), 1.1 nM (PDGFRα), 1.5 nM (VEGFR2), 2.2 nM (FGFR1), and 5.4 nM (Src).
- $50
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CitedBafetinib
Cited
T6311859212-16-1
Bafetinib (INNO-406) (INNO-406) is an effective and specific dual Bcr-Abl Lyn inhibitor (IC50: 5.8 19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR.
- $31
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CitedBGB-102
T10531807640-87-5
BGB-102 (JNJ-26483327) is a kinase inhibitor targeting FLT3 and YES1 and an antagonist targeting EGFR and VEGFR3, which may be useful in the study of macular degeneration and diseases associated with genetic disorders and malformations.
- $328
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A 419259 trihydrochloride
TQ01321435934-25-0In house
A 419259 trihydrochloride (RK 20449 trihydrochloride) is an Src family kinases inhibitor (IC50s: 9 nM, 3 nM and 3 nM for Src, Lck and Lyn).
- $48
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SGI-7079
T69821239875-86-5
SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance.
- $35
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PD173074 Cited
T2642219580-11-7
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 FGFR1 than PDGFR and c-Src.
- $36
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CitedTG 100801
T13157867331-82-6In house
TG 100801 is a dual inhibitor of VEGFr2 and Src family (Src and YES) kinases and is a candidate compound for the treatment of age-related macular degeneration (AMD).
- $84
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Tirbanibulin Cited
T6345897016-82-9
Tirbanibulin (KX2-391) is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibitor. KX2-391, belongs to an emerging new family of targeted cancer treatments called protein kinase inhibitors.
- $30
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CitedFenlean
T31773863193-70-8In house
Fenlean (FLZ) is a tyrosine kinase Src inhibitor, a synthetic cyclic derivative of squamous amide from Annona glabra, with cytoprotective activity, which protects tyrosine hydroxylase function in a chronic MPTP prostaglandin-type mouse model of Parkinson's disease.Fenlean inhibits the production of Aβ in the mitochondria, which may be useful in the study of age-related macular degeneration and Parkinson's disease. and Parkinson's.
- $119
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PP2 Cited
T6266172889-27-9
PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck Fyn (IC50:4 5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
- $39
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CitedDasatinib monohydrate Cited
T1448L863127-77-9
Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, Dasatinib monohydrate has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.
- $33
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CitedURMC-099
T60571229582-33-5
URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19 42 14 150 nM, for MLK1 MLK2 MLK3 DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
- $52
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Scutellarein Cited
T3319529-53-3
Scutellarein (6-Hydroxyapigenin) reduces inflammatory responses by inhibiting Src kinase activity.
- $110
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CitedNVP-BHG712
T6348940310-85-0
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
- $30
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Repotrectinib Cited
T40711802220-02-5
Repotrectinib (TPX-0005) is a potent ALK ROS1 TRK inhibitor, with IC50 values of 1.01 nM for WT ALK, 5.3 nM for SRC, 1.08 nM for ALK L1196M, and 1.26 nM for ALK G1202R.
- $45
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CitedCyt-PTPε Inhibitor-1
T10927428478-94-8In house
Cyt-PTPε Inhibitor-1 (A Inhibitor-1) is an inhibitor of cytosolic protein tyrosine phosphatase ε. Cyt-PTPε Inhibitor-1 blocks the dephosphorylation of c-Src and exhibits anti-osteoclastic activity.
- $35
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Lyn-IN-1
T11916887650-05-7
Lyn-IN-1 (Bafetinib analog) is a selective, potent dual inhibitor of Bcr-Abl and Lyn.
- $39
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UM-164
T4597903564-48-7
UM-164 (DAS-DFGO-II), a highly potent c-Src inhibitor with a dissociation constant (Kd) of 2.7 nM, also effectively inhibits p38α and p38β.
- $30
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AP23846
T68455878654-51-4In house
AP23846 is a novel and potent Src family kinase inhibitor that reduces vascular endothelial growth factor and interleukin-8 expression and abrogates downstream angiogenic processes in human solid tumor cell lines.
- $293
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LCB 03-0110 dihydrochloride
T326131962928-28-4In house
LCB 03-0110 Dihydrochloride is a potent inhibitor of the c-Src kinase (IC50 = 1.3 nM) and tyrosine kinases in the BTK and SYK family, as well as in the DDR2 family. It inhibits LPS-induced activation of macrophages and TGF-β1-induced activation of fibroblasts in vitro, inhibits activation of macrophages and fibroblasts, and inhibits scarring in wound healing models.
- $71
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Beta-Hydroxyisovalerylshikonin
TN14407415-78-3
Beta-Hydroxyisovalerylshikonin is an inhibitor of protein-tyrosine kinases such as v-Src and EGFR, and has been shown to induce apoptosis in several human tumor cell lines. Beta-Hydroxyisovalerylshikonin significantly decreased viability of HCT116 cells (IC50 values = 30.9 μg mL).
- $139
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Bosutinib Cited
T0152380843-75-4
Bosutinib (SKI-606) is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl (IC50: 1 nM) and Src (IC50: 1.2 nM) kinases.
- $33
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CitedPelitinib Cited
T2327257933-82-7
Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
- $43
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CitedA-443654
T14072552325-16-3
A-443654, a pan-Akt inhibitor, exhibits equal potency against Akt1, Akt2, and Akt3 within cells (Ki=160 pM).
- $84
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Rebastinib Cited
T26401020172-07-9
DCC-2036 (Rebastinib (DCC-2036)) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit. Rebastinib aimed at the Angiopoietin2-Tie2 pathway.
- $40
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CitedAZ12672857
T9650945396-55-4In house
AZ12672857 is an inhibitor of EphB4 with IC50 of 1.3 nM. AZ12672857 inhibits cell proliferation of Src transfected 3T3 cells with IC50 of 2 nM and autophosphorylation of EphB4 in transfected CHO-K1 cells with IC50 of 9 nM.
- $64
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Tolimidone
T689641964-07-2
Tolimidone (NSC 314335) is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals.
- $43
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Ponatinib Hydrochloride
T2372L1114544-31-8
Ponatinib Hydrochloride (AP-24534 Hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
- $39
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AD80 Cited
T43011384071-99-1
AD80, a multikinase inhibitor, targets RET, RAF, SRC, and S6K with significantly reduced activity on mTOR.
- $39
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CitedPF 477736
T6028952021-60-2
PF 477736 (PF-736,PF-00477736) is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.
- $45
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CGP77675
T30855234772-64-6In house
CGP77675 (ZINC1488120) is a potent and selective inhibitor of Src family kinase with IC50s of 5-20 and 40 nM for the phosphorylation of peptide substrates and autophosphorylation of purified Src. CGP77675 exhibits anticancer activity.
- $43
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SU6656
T6997330161-87-0
SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
- $34
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SB 203580 hydrochloride
T21675869185-85-3
SB 203580 hydrochloride (Adezmapimod hydrochloride) is a selective, ATP-competitive p38 MAPK inhibitor that induces mitochondrial autophagy and cytosolic autophagy and inhibits SAPK2a p38, SAPK2b p38β2, LCK, GSK3β, and PKBα. SB 203580 hydrochloride has been shown to be useful in antiretroviral therapy. 203580 hydrochloride inhibits amphoteric mechanical anomalous pain in a mouse model of antiretroviral-induced neuropathic pain.
- $36
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1-Naphthyl PP1
T3935221243-82-9
1-Naphthyl PP1 (1-NA-PP 1) is a selective Src inhibitor, targeting v-Src and c-Fyn, c-Abl, CDK2, and CAMK II with IC50 values of 1.0, 0.6, 0.6, 18, and 22 μM, respectively.
- $35
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lavendustin C
T4185125697-93-0
lavendustin C (NSC 666251) is a potent inhibitor of epidermal growth factor (EGF) receptor-associated tyrosine kinase.
- $37
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CHIR-124
T6350405168-58-3
CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2, 000-fold selectivity against Chk2, 500- to 5, 000-fold less activity against Cdc2 and CDK2 4.
- $35
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WH-4-023
T1811837422-57-8
WH-4-023 (Dual LCK SRC inhibitor) is a potent and orally active Lck Src inhibitor. It also potently inhibits SIK.
- $47
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Masitinib mesylate
T85441048007-93-7
Masitinib mesylate (AB-1010 mesylate) is a selective, orally bioavailable c-Kit inhibitor with an IC50 of 200 nM for human recombinant c-Kit, and IC50 values of 540 800 nM and 510 nM for PDGFRα β and LynB, respectively.
- $30
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Rigosertib
T16750592542-59-1
Rigosertib (ON-01910) is a selective, non-ATP-competitive PLK1 inhibitor (IC50: 9 nM) and multi-kinase inhibitor. As a selective anti-cancer agent, Rigosertib induces apoptosis by inhibiting the PI3 kinase Akt pathway, promotes histone H2AX phosphorylation, and induces G2 M arrest in the cell cycle.
- $34
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Agerafenib
T20701188910-76-0
Agerafenib (CEP32496) is a highly potent inhibitor of BRAF.
- $35
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