DCC-2618 Chemical Properties

Boiling point:

729.7±60.0 °C(Predicted)

Density 

1.40±0.1 g/cm3 (20 ºC 760 Torr)

storage temp. 

Store at -20°C

solubility 

DMF: 20 mg/ml; DMF:PBS (pH 7.2) (1:5): 0.1 mg/ml; DMSO: 14 mg/ml; Ethanol: Partially soluble

pka

12.10±0.70(Predicted)

form 

Powder

color 

White to off-white

DCC-2618 Usage And Synthesis

Biological Activity

DCC-2618 is an orally active, potent type II switch pocket (SP) inhibitor against c-KIT (IC50 = 4 nM/WT, 8 nM/V654A, 18 nM/T670I, 5 nM/D816H, 14 nM/D816V) and PDGFR. DCC-2618 locks c-KIT & PDGFR in an inactive conformation and is effective against multiple clinical forms of mutations resistant to type I ATP (catalytic)-site inhibitors Imatinib and Sunitinib. DCC-2618 inhibits cellular c-KIT activation (IC50 = 36 nM/WT, 2 nM/ex 11 del, 7 nM/ex 11 del & V654A, 53 nM/V560D & D820A) and is efficacious against KIT mutants-mediated cancer growth in cultres (IC50 = 2 nM; GIST with KIT D816Y) and in mice in vivo (50 mg/kg b.i.d. p.o.; GIST with KIT delW557K558/Y823D, AML with KIT N822K).

target

wt c-KIT