DCC-2618

Short Summary : C-Kit/PDGFR inhibtor

Category : Tyrosine Kinase|PDGFR

Purity : 0.9822

CAS Number : 1225278-16-9

Formula : C26H21F2N5O3

Molecular Weight : 489.47

SMILE : CN1C=C(C=N1)C2=NC=CC(=C2)OC3=C(C=C(C(=C3)F)NC(=O)C4(CC4)C(=O)NC5=CC=CC=C5)F

Solubility : >179.2mg/mL in DMSO

Storage : Store at -20°C

Description : IC50: 6 nM, 9 nM, 18 nM, 5 nM, 14 nM and 9 nM for wt c-KIT, KIT V654A, KIT T670I, KIT D816H, KIT D816V and KIT JMD VV/D816V, respectively. DCC-2618 is a small-molecule inhibitor of KIT kinases. Gastrointestinal stromal tumors (GIST) are driven by gain-of-function mutations of the KIT (approx 90%) or PDGFR (approx 10%) receptor tyrosine kinases. DCC-2618 has been designed to effectively inhibit the imatinib and sunitinib-sensitive KIT juxtamenbrane domin mutants as well as secondary resistant KIT iniase-domain mutants. In vitro: DCC-2618 is a kinase switch inhibitor that can control drug resistant mutants of KIT and PDGFR in GIST. DCC-2618 acts by imposing an inactive conformation (shape) of highly resistant and aggressive secondary mutations of KIT kinase [1]. In vivo: DCC-2618 inhibits KIT in GIST tumor xenografts after single dose. At the doses of 50 and 25 mpk, DCC-2618 showed promising potency on pKIT (Y703) with the inhibition ranging from 39% to 79% 2-12 hrs after the administration [1]. Clinical trial: A Phase I trial with refractory GIST patients is planned.Reference:[1] DCC-2618, a small molecule inhibitor of normal and mutant KIT kinasefor treatment of refractory gastrointestinal stromal tumors (GIST)Deciphera Pharmaceuticals, Lawrence, KS.

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