A c-Kit and PDGFRα inhibitor (IC50s = 13

DCC-2618 – 10 mg

Brand:
Cayman
CAS:
1225278-16-9
Storage:
-20
UN-No:
Non-Hazardous - /

DCC-2618 is a type II inhibitor of wild-type and mutant c-Kit and PDGFRα (IC50s = 13, 11, 9.2, 18, 25, 3.6, and 36 nM for c-Kit, c-KitV654A, c-KitT670I, c-KitD816H, c-KitD816V, PDGFRα, and PDGFRαD842V, respectively).{53053} It also inhibits DDR2, VEGFR2, PDGFRβ, and Tie2 (IC50s = 50s = 50s = 2.3-229 and 1.9-56 nM, respectively). It also inhibits proliferation of HMC-1, ROSA, and MCPV-1 mast cells, as well as neoplastic mast cells isolated from patients with advanced systemic mastocytosis (IC50s = In vivo, DCC-2618 (25 and 100 mg/kg) inhibits c-Kit phosphorylation and reduces tumor burden in a GISTT1 lung cancer mouse xenograft model.{53053}  

 

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SKU: 26174 - 10 mg Category:

Description

A c-Kit and PDGFRα inhibitor (IC50s = 13, 11, 9.2, 18, 25, 3.6, and 36 nM for c-Kit, c-KitV654A, c-KitT670I, c-KitD816H, c-KitD816V, PDGFRα, and PDGFRαD842V, respectively); inhibits DDR2, VEGFR2, PDGFRβ, and Tie2 (IC50s = 50s = 50s = 2.3-229 and 1.9-56 nM, respectively); inhibits proliferation of HMC-1, ROSA, and MCPV-1 mast cells, as well as neoplastic mast cells isolated from patients with advanced systemic mastocytosis (IC50s = <1 μM); inhibits c-Kit phosphorylation and reduces tumor burden in a GISTT1 lung cancer mouse xenograft model at 100 mg/kg

Formal name: N-[2,5-difluoro-4-[[2-(1-methyl-1H-pyrazol-4-yl)-4-pyridinyl]oxy]phenyl]-N’-phenyl-1,1-cyclopropanedicarboxamide

Synonyms:  Ripretinib

Molecular weight: 489.5

CAS: 1225278-16-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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