c-Kit-IN-1 产品说明书 Chemicals
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产品编号 DC9585
名称 c-Kit-IN-1

化学性质

CAS 1225278-16-9
分子式 C26H21F2N5O3
分子量 489.4734
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description CAS NO.:1225278-16-9
Product Name:
Synonyms:
EINECS:
Molecular Formula:C26H21F2N5O3
Molecular Weight:489.4734
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


DCC-2618 is a small molecule inhibitor of c-Kit and PDGFR with IC50s of 6 nM/30 nM/13 nM for c-Kit/PDGFRα/PDGFRβ respectively. in vitro: DCC-2618 inhibits normal and mutant KIT kinase at the nanomol level. The targets are wt c-KIT, c-KIT mutants, PDGFR alpha, PDGFR beta, KDR and cFMS. DCC-2618 inhibits mutant KIT in GIST patient cell line (GIST T1 pKIT western Ex11 deletion) at a IC 50 of 2 nM. Deciphera's technology has identified DCC-2618 as a molecule which can be developed as second line therapy for imatinib and sunitinib resistant GIST patients with the potential to progress to frontline GIST therapy. DCC-2618 has been designed to effectively inhibit the imatinib and sunitinib-sensitive KIT juxtamembrane domain mutants (JMD) as well as secondary resistant KIT kinase-domain mutants. DCC-2618 additionally targets PDGFR alpha oncogenic mutants.
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