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(79)
Angiogenesis Filter
Angiogenesis Tyrosine Kinase/AdaptorsACK
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ALK
(79)
BTK
(85)
Bcr-Abl
(79)
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(19)
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(26)
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(12)
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(326)
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(39)
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(49)
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(9)
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(59)
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(61)
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(243)
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(43)
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.
Lenvatinib
Cited
T0520417716-92-8
Lenvatinib (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
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QTY
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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CitedAvapritinib
T51091703793-34-3
Avapritinib (BLU-285) is a selective, highly potent, and orally active inhibitor of KIT and PDGFRA activation loop mutant kinases, targeting KIT D816V (IC50:0.27 nM) and PDGFRA D842V (IC50:0.24 nM), and attenuates the transport functions of ABCB1 and ABCG2. It binds to the active conformation of the kinases and exhibits antitumor activity.
- $80
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Sorafenib Cited
T0093L284461-73-0
Sorafenib (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
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CitedRegorafenib Cited
T1792755037-03-7
Regorafenib (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
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CitedImatinib Mesylate Cited
T1621220127-57-1
Imatinib 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
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CitedCrenolanib
Cited
T2677670220-88-9
Crenolanib (ARO 002) is an orally bioavailable type III tyrosine kinases inhibitor of PDGFRα β and FLT3 (IC50s: 11, 3.2, and 4 nM).
- $53
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CitedMethylnissolin
TN235473340-41-7
Methylnissolin 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
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Axitinib Cited
T1452319460-85-0
Axitinib (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
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CitedNintedanib esylate
T5001656247-18-6
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor targeting VEGFR1 2 3, FGFR1 2 3, and PDGFRα β.
- $36
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Lenvatinib mesylate Cited
T8541857890-39-2
Lenvatinib mesylate (E7080 (mesylate)) is an oral and multi-targeted inhibitor of VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, with potent antitumor activities.
- $34
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CitedCP-673451 Cited
T6091343787-29-1
CP-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
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CitedRipretinib
T84821442472-39-0
Ripretinib (DCC-2618) is an orally bioavailable inhibitor of (KIT) and (PDGFRA).
- $419
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Ponatinib 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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CitedDovitinib
T6289405169-16-6
Dovitinib is an orally active, multi-targeted tyrosine kinase (RTK) inhibitor with anti-tumor effects.
- $39
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Vorolanib
T84911013920-15-4
Vorolanib (X-82) is an orally active VEGFR PDGFR dual inhibitor.
- $115
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Imatinib Cited
T6230152459-95-5
Imatinib (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
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CitedSunitinib Cited
T0374L557795-19-4
Sunitinib (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
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CitedSennoside B
T2734128-57-4
Sennoside B is an anthranoid. Anthranoid derivatives are used all over the world as a treatment for constipation.
- $60
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Dovitinib lactate hydrate
T6479915769-50-5
Dovitinib 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
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Pazopanib
T0097L444731-52-6
Pazopanib (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
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Dovitinib lactate
T7104692737-80-7
Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).
- $47
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Bisindolylmaleimide I Cited
T6513133052-90-1
Bisindolylmaleimide I (GF109203X) is a potent and highly selective protein kinase C (PKC) inhibitor, exhibiting a Ki of 14 nM.
- $61
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CitedKi20227
T4315623142-96-1
Ki-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
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Ilorasertib
TQ00591227939-82-3
Ilorasertib (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).
- $33
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AXL-IN-13
T733002376928-82-2In house
AXL-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
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Linifanib
T2514796967-16-3
Linifanib (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
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Cediranib Cited
T2500288383-20-0
Cediranib (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
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CitedChiauranib
T355701256349-48-0
Chiauranib 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
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Sorafenib tosylate Cited
T0093475207-59-1
Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6 20 22 nM for Raf-1 VEGFR-3 B-Raf).
- $37
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CitedTyrphostin A9
T247910537-47-0
Tyrphostin A9 (SF 6847) is an Agricultural acaricide, now superseded. Tyrphostin A9 is firstly designed as an EGFR inhibitor
- $42
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Pazopanib Hydrochloride
T6930635702-64-6
Pazopanib Hydrochloride (Votrient HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively.
- $48
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XL 999
T5466705946-27-6
Tyrosine 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
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PD-089828
T8976179343-17-0
PD 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
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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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Regorafenib Hydrochloride
T8402835621-07-3
Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
- $30
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Tivozanib
T2456475108-18-0
Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.
- $34
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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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Masitinib
T2609790299-79-5
Masitinib (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
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PDGFRα kinase inhibitor 1
T123962209053-93-8
PDGFRα 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
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Mubritinib Cited
T6124366017-09-6
Mubritinib (TAK-165) (TAK-165) is a potent inhibitor of HER2 ErbB2 with IC50 of 6 nM.
- $208
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CitedPonatinib 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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Telatinib
T6166332012-40-5
Telatinib (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.
- $33
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SU 5402
T6996215543-92-3
SU 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
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Sunitinib Malate
T0374341031-54-7
Sunitinib 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
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AG-1478 Cited
T2047153436-53-4
AG-1478 (NSC-693255) (Tyrphostin AG-1478) is a selective EGFR inhibitor.
- $45
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CitedCP-547632
T10870L252003-65-9In house
CP-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
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N-(p-Coumaroyl) serotonin
TN196968573-24-0
N-(p-Coumaroyl) Serotonin, a polyphenol isolated from the seeds of safflower, exhibits antioxidant, cardioprotective effects after ischemia, and antitumor activity. It may improve vascular distensibility and reduce cardiovascular risk. N-(p-Coumaroyl) Serotonin ameliorates atherosclerosis and distensibility of the aortic wall in vivo, and is commonly used in atherosclerosis research.
- $36
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