Cat.No. | Name | Information |
---|---|---|
M4867 | Pexidartinib | Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit, and Flt3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. |
M3241 | Imatinib | Imatinib is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM, respectively. |
M25163 | Barzolvolimab | Barzolvolimab (CDX 0159) is a humanized anti-KIT IgG1 monoclonal antibody. Barzolvolimab specificity and potently inhibits KIT activation by SCF. Barzolvolimab can reduce skin mast cells and disease activity in chronic inducible urticaria. |
M22464 | M4205 | M4205 is a c-KIT inhibitor, with an IC50 of 10 nM for c-KIT V654A. M4205 has high activity on c-KIT mutations in exon 11, 13, 17. |
M20646 | AZD3229 | AZD3229 is a potent, pan-KIT mutant inhibitor with potent single digit nM growth inhibition against a diverse panel of mutant KIT driven Ba/F3 cell lines (GI50=1-50 nM), with good margin to KDR-driven effects. It also inhibits PDGFR mutants (Tel-PDGFRα, Tel-PDGFRβ, V561D/D842V). |
M10665 | Masitinib mesylate | Masitinib (AB-1010) mesylate is a potent, orally bioavailable and selective inhibitor of c-Kit, IC50 of 200 nM for human recombinant c-Kit. It also inhibits PDGFRα/β, LynB with IC50 values of 540, 800 and 510 nM. |
M9903 | Ripretinib | Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFR-alpha inhibitor. |
M5329 | Motesanib | Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. |
M43484 | Labuxtinib | Labuxtinib is c-kit tyrosine kinase inhibitor. |
M29836 | Elenestinib phosphate | Elenestinib phosphate (BLU-263 phosphate) is a potent and orally active tyrosine kinase inhibitor. Elenestinib phosphate has the potential for the research of systemic mastocytosis (SM). |
M29682 | Elenestinib | Elenestinib (BLU-263) is a potent and orally active tyrosine kinase inhibitor. Elenestinib has the potential for the research of systemic mastocytosis (SM). |
M28692 | Bezuclastinib | Bezuclastinib (CGT9486; PLX 9486) is a potent inhibitor of c-kit and c-kit D816V (0.0001 < IC50 < 1 μM). Bezuclastinib is a tyrosine kinase inhibitor. |
M27723 | Amuvatinib hydrochloride | Amuvatinib hydrochloride (MP470 hydrochloride) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib hydrochloride (MP470 hydrochloride) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity. |
M27604 | c-Kit-IN-5-1 | c-Kit-IN-5 is potent inhibitor of c-Kit, with IC50s of 22 nM and 16 nM in kinase assay and cell assay, respectively. c-Kit-IN-5 shows more than 200-fold selectivity for c-Kit over KDR, p38, Lck, and Src. c-Kit-IN-5 also exhibits desirable pharmacokinetic properties. |
M20635 | DCC-2618 | DCC-2618 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of KIT and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. |
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