Biochem/physiol Actions
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).
Orally active, potent type II switch pocket (SP) c-KIT & PDGFR inhibitor against multiple clinical forms of mutations resistant to Imatinib and Sunitinib.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | O=C(NC1=CC=CC=C1)C2(CC2)C(NC(C=C3F)=C(F)C=C3OC4=CC(C5=CN(C)N=C5)=NC=C4)=O |
| InChI | 1S/C26H21F2N5O3/c1-33-15-16(14-30-33)21-11-18(7-10-29-21)36-23-13-19(27)22(12-20(23)28)32-25(35)26(8-9-26)24(34)31-17-5-3-2-4-6-17/h2-7,10-15H,8-9H2,1H3,(H,31,34)(H,32,35) |
| InChI key | WWOXKWLDMLMYQY-UHFFFAOYSA-N |
