| Cat. No. |
Product Name |
CAS No. |
Information |
| H8089 |
Brivanib alaninate
|
649735-63-7 |
A prodrug of Brivanib, which is a dual inhibitor of VEGFR2 and FGFR1 with IC50 of 25 nM and 148 nM respectively; exhibits improved aqueous solubility and oral bioavailability of the parent compound. |
| H8088 |
Brivanib
|
649735-46-6 |
A dual inhibitor of VEGFR2 and FGFR1 with IC50 of 25 nM and 148 nM respectively; shows weak activity for VEGFR1 (IC50=380 nM), and no significant activity on EGFR, PDGFRβ, Lck, etc.; demonstrates robust in vivo activity in human tumor xenograft models. |
| H7935 |
Linsitinib
|
867160-71-2 |
Linsitinib (ASP-7487, OSI-906) is a potent, selective, orally active, dual IGF-1R/insulin receptor inhibitor with IC50 of 35/75 nM, respectively; potently and selectively inhibits autophosphorylation of both human IGF-1R and IR, displays in vitro antiproliferative effects in a variety of tumor cell lines and shows robust in vivo anti-tumor efficacy in an IGF-1R-driven xenograft model.
|
| H7878 |
H3B-6527
|
1702259-66-2 |
A potent, highly selective covalent FGFR4 inhibitor with IC50 of 10,000, and >10,000 nM); inhibits Hep3B celll viability with GI50 of 25 nM in ATP-based cell viability assay, inhibits proliferation and leads to apoptosis in HCC cell lines by inhibiting FGFR4 signaling; exhibits antitumor activity in the Hep3B human HCC xenograft mouse model. |
| H7874 |
FGF-401
|
1708971-55-4 |
FGF-401 (NVP-FGF401, Roblitinib, FGF401)?is a first-in-class, potent, highly selective FGFR4 inhibitor with IC50 of 1.1 nM; shows >1,000-fold selectivity against of panel of 65 kinases and in a kinome of 456 kinases; potently inhibits phospho-FGFR4 in vivo, exhibits anti-tumor activity in s several xenograft animal models. |
| H7868 |
Derazantinib
|
1234356-69-4 |
Derazantinib (ARQ-087) is a novel potent, ATP competitive multi-kinase inhibitor with IC50 of FGFR1/2/3 with IC50 of 1.8-4.5 nM; also inhibits FGFR4, Src, Abl, RET, etc. (IC50<50 nM); inhibits FGFR2 auto-phosphorylation and other proteins downstream in the FGFR pathway (FRS2α, AKT, ERK), shows potent anti-proliferative effect in cell lines driven by FGFR dysregulation; shows tumor growth inhibition in vivo in xenograft tumor models. |
| H7865 |
BLU-554
|
1707289-21-1 |
BLU-554 (Fisogatinib, BLU554) is a novel potent, highly selective and orally bioavailable inhibitor of FGFR4 designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation; targets FGFR4 while sparing other members of the FGFR family and showing little to no inhibition of all other kinases.
|
| H7761 |
Tivantinib
|
905854-02-6 |
Tivantinib (ARQ-197) is a potent, selective, non-ATP-competitive inhibitor of c-Met with Ki of 355 nM; has no inhibition for EGFR, InsR, PDGFRα, FGFR1 and FGFR4 etc., only modest inhibition (35%) for Ron at 30 uM; inhibits constitutive c-Met phosphorylation in HT29 and MKN-45 cells, and HGF-induced c-Met phosphorylation in MDA-MB-231 and NCI-H441 cells with IC50 of 100-300 nM; shows antiproliferative activity against multiple cancer cell lines (IC50=0.03-30 uM); exerts tumor growth inhibition in multiple mouse xenograft; orally active.
|
| H7760 |
Tepotinib
|
1100598-32-0 |
Tepotinib (EMD-1214063)?is a potent and highly selective c-Met inhibitor with IC50 of 3 nM; shows selectivity versus a panel of 242 human kinases; inhibits c-Met phosphorylation and downstream signaling in a dose-dependent fashion; induces regression of human tumors in murine xenograft models.
|
| H7755 |
PLB-1001
|
1440964-89-5 |
PLB-1001 (Bozitinib, PLB1001, CBI-3103, CBT-101) is a potent, highly selective, ATP-competitive, BBB-permeable MET kinase inhibitor, potently inhibits MET activity by 95.1% at 2 uM; Similar with crizotinib, PLB-1001 inhibited the phosphorylation of MET and STAT3, indicating a robust inhibitory effect of PLB-1001 on MET and its downstream signaling pathways; demonstrates remarkable potency in selectively inhibiting MET-altered tumor cells (METex14) in preclinical models; also exhibits clinical potential for precisely treating gliomas.
|
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