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Angiogenesis
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Angiogenesis Tyrosine Kinase/AdaptorsACK
(5)
ALK
(77)
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(82)
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(78)
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(55)
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PDGFR
Platelet-derived growth factor receptors (PDGF-R) are cell surface tyrosine kinase receptors for members of the platelet-derived growth factor (PDGF) family. PDGF subunits -A and -B are important factors regulating cell proliferation, cellular differentiation, cell growth, development and many diseases including cancer. There are two forms of the PDGF-R, alpha and beta each encoded by a different gene. Depending on which growth factor is bound, PDGF-R homo- or heterodimerizes.
- NintedanibT1777656247-17-5Nintedanib (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
SizeQTY
Cited - LenvatinibT0520417716-92-8Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.
- $40
SizeQTY Cited - RegorafenibT1792755037-03-7Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity.
- $30
SizeQTY
Cited - SorafenibT0093L284461-73-0Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6 22 90 15 20 20 57 58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.
- $34
SizeQTY Cited - AvapritinibT51091703793-34-3Avapritinib (BLU-285) is a dual inhibitor targeting the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).
- $80
SizeQTY - DovitinibT6289405169-16-6Dovitinib (CHIR-258) (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3 c-Kit, IC50: 1 2 nM), also effective to class IV (FGFR1 3) and class V (VEGFR1-4) RTKs (IC50: 8-13 nM), less potent to EGFR, InsR, EphA2, c-Met, IGF-1R, Tie2, and HER2.
- $39
SizeQTY
- Imatinib MesylateT1621220127-57-1Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).
- $54
SizeQTY Cited - CrenolanibT2677670220-88-9Crenolanib (ARO 002) is an orally bioavailable type III tyrosine kinases inhibitor of PDGFRα β and FLT3 (IC50s: 11, 3.2, and 4 nM).
- $53
SizeQTY Cited - PonatinibT2372943319-70-8Ponatinib (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
SizeQTY Cited - CP-673451T6091343787-29-1CP-673451 is a specific inhibitor of PDGFRα β (IC50: 10 1 nM) with antiangiogenic and antitumor activity and the selectivity is higher 450-fold than other angiogenic receptors.
- $44
SizeQTY Cited - Nintedanib esylateT5001656247-18-6Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor targeting VEGFR1 2 3, FGFR1 2 3, and PDGFRα β.
- $36
SizeQTY - Lenvatinib mesylateT8541857890-39-2Lenvatinib mesylate (E7080 (mesylate)) is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.
- $34
SizeQTY Cited - MethylnissolinTN235473340-41-7Methylnissolin is a natural product isolated from Astragalus membranaceus that inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. It inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibiting the ERK1/2 MAP kinase cascade. It also inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinases and has antibacterial and anticancer effects.
- $81
SizeQTY - SunitinibT0374L557795-19-4Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80 2 nM). It exhibits antitumor activity and is used for treating kidney cancer and gastrointestinal tumors.
- $53
SizeQTY Cited - ImatinibT6230152459-95-5Imatinib (STI571) is a multi-targeted receptor tyrosine kinase inhibitor that selectively inhibits the kinase activities of BCR ABL, v-Abl, PDGFR, and c-kit with oral activity. Imatinib has antitumor activity for the treatment of chronic granulocytic leukemia.
- $36
SizeQTY Cited - RipretinibT84821442472-39-0Ripretinib (DCC-2618) is an orally bioavailable inhibitor of (KIT) and (PDGFRA).
- $68
SizeQTY - AxitinibT1452319460-85-0Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4 20 0.4 2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.
- $33
SizeQTY Cited - PazopanibT0097L444731-52-6Pazopanib (GW786034) is an inhibitor of protein tyrosine kinases that inhibits VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms (IC50=10 30 47 84 74 140 146 nM). Pazopanib has antitumor activity.
- $42
SizeQTY - LinifanibT2514796967-16-3Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).
- $43
SizeQTY - VorolanibT84911013920-15-4Vorolanib (X-82) is an orally active VEGFR/PDGFR dual inhibitor.
- $115
SizeQTY - Dovitinib lactateT7104692737-80-7Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).
- $47
SizeQTY - Ki20227T4315623142-96-1Ki-20227 is a specific c-Fms tyrosine kinase(CSF1R) inhibitor (IC50: 2 nM). It also has certain inhibitory against VEGFR2(IC50: 12 nM) and c-Kit PDGFRβ(IC50: 451 217 nM), respectively.
- $39
SizeQTY - Dovitinib lactate hydrateT6479915769-50-5Dovitinib lactate hydrate (TKI258) is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3 c-Kit) with IC50 of 1 nM 2 nM, also potent to class IV (FGFR1 3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
- $50
SizeQTY - Bisindolylmaleimide IT6513133052-90-1Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM.
- $61
SizeQTY Cited - AXL-IN-13T733002376928-82-2In houseAXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 of 1.6 nM and a Kd of 0.26 nM. It exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion.
- $79
SizeQTY - IlorasertibTQ00591227939-82-3Ilorasertib (ABT-348) (ABT-348) is an ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora A Aurora B Aurora C (IC50s: 120 nM 7 nM 1 nM). It also suppresses RET tyrosine kinase, PDGFRβ, and Flt1 (IC50s: 7 nM, 3 nM, and 32 nM).
- $55
SizeQTY - Sorafenib tosylateT0093475207-59-1Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).
- $37
SizeQTY Cited - CediranibT2500288383-20-0Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.
- $35
SizeQTY Cited - ChiauranibT355701256349-48-0Chiauranib is a multi-target inhibitor against tumor angiogenesis and exhibits potent anticancer effects. Chiauranib potently inhibits the angiogenesis-related kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-related kinase Aurora B, and chronic inflammation-related kinase CSF1R, with IC50 values ranging from 1-9 nM.
- $83
SizeQTY - PDGFRα kinase inhibitor 1T123962209053-93-8PDGFRα kinase inhibitor 1 is a highly selective inhibitor of type II PDGFRα kinase (PDGFRα and PDGFRβ) with IC50 values of 132 nM and 6115 nM, respectively.
- $399
SizeQTY - Tyrosine kinase-IN-1T5466705946-27-6Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor that acts on KDR, Flt-1, FGFR1, and PDGFRα with IC50 values of 4 nM, 20 nM, 4 nM, and 2 nM, respectively.
- $35
SizeQTY - PD-089828T8976179343-17-0PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 µM)
- $31
SizeQTY - TivozanibT2456475108-18-0Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.
- $34
SizeQTY - RigosertibT16750592542-59-1Rigosertib (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
SizeQTY - Regorafenib HydrochlorideT8402835621-07-3Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
- $30
SizeQTY - Tyrphostin A9T247910537-47-0Tyrphostin A9 (SF 6847) is an Agricultural acaricide, now superseded. Tyrphostin A9 is firstly designed as an EGFR inhibitor
- $42
SizeQTY - CHIR-124T6350405168-58-3CHIR-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
SizeQTY - MasitinibT2609790299-79-5Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.
- $31
SizeQTY - TelatinibT6166332012-40-5Telatinib (Bay 57-9352) is an effective inhibitor of VEGFR2 3, c-Kit, and PDGFRα, with IC50s of 6 nM 4 nM, 1 nM, and 15 nM, respectively.
- $39
SizeQTY - ENMD-2076T2358934353-76-1ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
- $47
SizeQTY - TAK-632T18861228591-30-7TAK-632, a potent pan-Raf inhibitor (GenScript, 2020), is characterized by its molecular weight [M] for [C 22 H 19 FN 2 O 2] of 362.4 by LC-MS, with a purity of 99% (HPLC). The compound exhibits white to off-white solid form and has a melting point [M] ranging from 178°C to 182°C (GenScript, 2020). Its solubility profile includes DMSO, in which it is soluble to 100mM (GenScript, 2020).
- $35
SizeQTY Cited - AG-1478T2047153436-53-4AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.
- $45
SizeQTY Cited - MubritinibT6124366017-09-6Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2 ErbB2 with IC50 of 6 nM.
- $32
SizeQTY Cited - SU 5402T6996215543-92-3SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 values of 20 nM for VEGFR2, 30 nM for FGFR1, and 510 nM for PDGF-Rβ.
- $59
SizeQTY - Sennoside BT2734128-57-4Sennoside B is an anthranoid. Anthranoid derivatives are used all over the world as a treatment for constipation.
- $60
SizeQTY - ZM323881 hydrochlorideT1991193000-39-4In houseZM323881 hydrochloride (ZM 323881 HCl) is a potent and selective VEGFR2 inhibitor.
- $66
SizeQTY Cited - CP-547632T10870L252003-65-9In houseCP-547632 is an orally available and potent, ATP-competitive dual inhibitor of VEGFR-2 and FGF kinase F with IC50s of 11 nM and 9 nM, respectively. CP-547632 is selective, with higher selectivity for VEGFR2 and bFGF than for EGFR, PDGFRβ and related tyrosine kinases (TKs). PDGFRβ and related tyrosine kinases (TKs) CP-547632 has antitumour activity.
- $30
SizeQTY - GNF-5837T60971033769-28-6GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA TrkB (IC50: 8 12 nM).
- $43
SizeQTY Cited - KI8751T2446228559-41-9KI8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM.
- $31
SizeQTY - FlumatinibT4320895519-90-1Flumatinib (HHGV678) is an orally bioavailable tyrosine kinase inhibitor with potential antineoplastic activity.
- $30
SizeQTY
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