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Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFR-alpha inhibitor. Ripretinib (DCC-2618) suppresses phosphorylation of KIT and decreases the expression of phosphosphorylated (p)STAT5, pAKT and pERK1/2 in neoplastic mast cells.
| Molecular Weight | 510.36 |
| Formula | C24H21BrFN5O2 |
| CAS Number | 1442472-39-0 |
| Solubility (25°C) | DMSO 32 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Cancer Discov. BLU-285, DCC-2618 Show Activity against GIST
| Related c-Kit Products |
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| 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. |
| 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. |
| 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. |
| 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. |
| 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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Products are for research use only. Not for human use. We do not sell to patients.
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