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Angiogenesis
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Angiogenesis Tyrosine Kinase/AdaptorsACK
(5)
ALK
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Bcr-Abl
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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.
- SorafenibT0093L284461-73-0Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits 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. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.
- $34
SizeQTY
Cited - RegorafenibT1792755037-03-7Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
- $30
SizeQTY Cited - AvapritinibT51091703793-34-3Avapritinib (BLU-285) is a dual inhibitor of the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM).
- $80
SizeQTY - 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 - PazopanibT0097L444731-52-6Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.
- $42
SizeQTY - Sennoside BT2734128-57-4Sennoside B is an anthranoid. Anthranoid derivatives are used all over the world as a treatment for constipation.
- $60
SizeQTY - 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 - 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 - Imatinib impurities3T67847404844-11-7Imatinib impurities3 is a protein kinases inhibitor with IC50 values of 6.95uM, 0.245uM, 0.139uM for ABL1 wt, KIT wt, PDGFRR wt, respectively.
- $40
SizeQTY
- KN1022T60110205255-11-4KN1022 is an inhibitor of phosphorylation of platelet-derived growth factor (PDGF) receptor with IC50 of 0.26 μM.
- $117
SizeQTY - N-Desethylsunitinib hydrochlorideT12145L1261432-05-6N-Desethylsunitinib hydrochloride is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.
- $133
SizeQTY - ZM323881 hydrochlorideT1991193000-39-4In houseZM323881 hydrochloride (ZM 323881 HCl) is a potent and selective VEGFR2 inhibitor.
- $66
SizeQTY Cited - TG 100572 HydrochlorideT13156L867331-64-4In houseTG 100572 Hydrochloride is a inhibitor of multi-targeted kinase which inhibits receptor tyrosine kinases and Src kinases(IC50s of 2, 7, 2, 16, 13, 5, 0.5, 6, 0.1, 0.4, 1, 0.2 nM for VEGFR1, VEGFR2, FGFR1, FGFR2, PDGFRβ, Fgr, Fyn, Hck, Lck, Lyn, Src, Yes, respectively).
- $399
SizeQTY - AXL-IN-13T733002376928-82-2In houseAXL-IN-13 is a potent and orally active AXL inhibitor with an IC50 value of 1.6 nM and a Kd value of 0.26 nM.AXL-IN-13 exhibits anticancer activity, reverses TGF-β1-induced epithelial-mesenchymal transition (EMT) and inhibits cancer cell migration and invasion.
- $79
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 - PP121T24151092788-83-4PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
- $51
SizeQTY Cited - GNF-5837T60971033769-28-6GNF-5837 is a specific, and orally bioavailable pan-TRK inhibitor for TrkA TrkB (IC50: 8 12 nM).
- $43
SizeQTY Cited - 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 - AxitinibT1452319460-85-0Axitinib (AG-013736) is an orally bioavailable tyrosine kinase inhibitor with IC50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nM for VEGFR1, VEGFR2, VEGFR3, c-kit, and PDGFRβ, respectively.
- $33
SizeQTY Cited - Bisindolylmaleimide IT6513133052-90-1Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor with a Ki of 14 nM.
- $61
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 - MubritinibT6124366017-09-6Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2 ErbB2 with IC50 of 6 nM.
- $32
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 - 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 - OrantinibT6184252916-29-3Orantinib (NSC 702827) , a excellent effective against PDGFR autophosphorylation with Ki of 8 nM, also highly inhibits Flk-1 and FGFR1 trans-phosphorylation. It shows little effect against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2 and does not suppresses EGFR.
- $47
SizeQTY Cited - SunitinibT0374L557795-19-4Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.
- $53
SizeQTY Cited - 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 - 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 - AG-1478T2047153436-53-4AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.
- $45
SizeQTY Cited - AmuvatinibT2516850879-09-3Amuvatinib (MP470) is an orally bioavailable synthetic carbothioamide with potential antineoplastic activity.
- $44
SizeQTY Cited - PonatinibT2372943319-70-8Ponatinib (AP24534) is an orally available, multitargeted kinase inhibitor (IC50s: 0.37/1.1/1.5/2.2/5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively).
- $50
SizeQTY Cited - NVP-ACC789T3463300842-64-2ACC-789 (NVP-ACC789 (ZK202650); ZK-202650) is an effective, specific and orally active inhibitor of the VEGF receptor tyrosine kinases.
- $39
SizeQTY - KG5T41003877874-85-6KG5 is a dual allosteric inhibitor of PDGFRβ and B-Raf with a Kd of 520 nM and 300 nM for PDGFRβ and PDGFRα. KG5 inhibits FLT3, KIT, and c-Raf with anticancer and antiangiogenic activities.
- $48
SizeQTY - Multi-kinase inhibitor 1T4191778274-97-8Multi-kinase inhibitor 1 (Multi-kinase inhibitor I) is a Multi-kinase inhibitor.
- $33
SizeQTY - CT52923T60226205256-55-9CT52923 is a selective, orally active antagonist of platelet-derived growth factor receptor (PDGFR), functioning as an ATP-competitive inhibitor. It has versatile applications for researching an array of pathological diseases such as atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer.
- $30
SizeQTY - OlaratumabT767611024603-93-7Olaratumab(IMC-3G3) is a human monoclonal IgG1 antibody against platelet-derived growth factor receptor alpha (PDGFRα), which has antitumor effects and can be used to study advanced soft tissue sarcomas.
- $247
SizeQTY - Masitinib mesylateT85441048007-93-7Masitinib mesylate (AB-1010 mesylate) is a selective and orally bioavailable c-Kit inhibitor (IC50 of 200 nM,540/800 nM,510 nM for human recombinant c-Kit;PDGFRα/β;LynB,respectively).
- $30
SizeQTY - SU14813 maleateTQ0080849643-15-8SU14813 maleate is an inhibitor of multi-targeted receptor tyrosine kinases (IC50s: 2, 50, 4, 15 nM for VEGFR1, VEGFR2, PDGFRβ, and KIT).
- $53
SizeQTY - Tyrphostin AG1433T13238168835-90-3Tyrphostin AG1433 (AG1433) is an inhibitor of tyrosine kinases and also a dual inhibitor of PDGFRβ(IC50s = 5.0 μM) and VEGFR-2 (Flk-1/KDR)(IC50s = 9.3 μM).
- $44
SizeQTY - TrapidilT008015421-84-8Trapidil (Avantrin) is a coronary vasodilator agent. It was originally developed as a vasodilator and anti-platelet agent and has been used to treat patients with ischemic coronary heart, liver, and kidney disease.
- $42
SizeQTY - PD-161570T23127192705-80-9PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively.
- $98
SizeQTY - Regorafenib monohydrateT1792L1019206-88-2Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.
- $30
SizeQTY - SeralutinibT89001619931-27-9Seralutinib (GB002) is an inhibitor of inhaled PDGFRα and PDGFRβ. It is used in the study for pulmonary arterial hypertension.
- $42
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 - 5Z-7-OxozeaenolT14055253863-19-35Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.
- $215
SizeQTY - AC710TQ02351351522-04-7AC710 is a potent PDGFR inhibitor (Kds: 0.6, 1, 1.57, 1.3, 1 nM for FLT3, KIT, CSF1R, PDGFRα and PDGFRβ).
- $30
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 - Sunitinib MalateT0374341031-54-7Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.
- $37
SizeQTY
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