Avapritinib, Catalog: B2999

Alternate Names BLU-285; (1S)-1-(4-fluorophenyl)-1-[2-[4-[6-(1-methylpyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]piperazin-1-yl]pyrimidin-5-yl]ethanamine

Appearance White to off-White Solid Powder

CAS # 1703793-34-3

Molecular Formula C₂₆H₂₇FN₁₀

Molecular Weight 498.56

Purity > 98%

Solubility ~ 66 mg/ml in DMSO, ~ 3 mg/ml in Ethanol

SMILES CC(C1=CC=C(C=C1)F)(C2=CN=C(N=C2)N3CCN(CC3)C4=NC=NN5C4=CC(=C5)C6=CN(N=C6)C)N

InChi InChI=1S/C26H27FN10/c1-26(28,20-3-5-22(27)6-4-20)21-13-29-25(30-14-21)36-9-7-35(8-10-36)24-23-11-18(16-37(23)33-17-31-24)19-12-32-34(2)15-19/h3-6,11-17H,7-10,28H2,1-2H3/t26-/m0/s1

InChi Key DWYRIWUZIJHQKQ-SANMLTNESA-N

PubChem CID 118023034

MDL Number MFCD31544325

Storage Conditions -20ºC

Shipping Conditions RT

Usage For Research Use Only! Not For Use in Humans.

Handling Do not take it internally. Wear a glove and mask when handling the product. Protect from air and moisture.

Avapritinib is an inhibitor of oncogenic KIT and PDGFRA mutations. The KIT receptor belongs to the class III receptor tyrosine kinase (RTK) family. Avapritinib potently inhibits the activation loop mutants KIT D816V and PDGFRA D842V and also inhibits other well-characterized disease-driving KIT mutants. It inhibits KIT D816V and PDGFRA D842V with IC₅₀ values of 0.27 nM and 0.24 nM respectively. Avapritinib (0.3-30 mg/kg) reduces tumor volume in a P815 KIT D814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. It has showed marked activity in patients with diseases associated with KIT (aggressive systemic mastocytosis and gastrointestinal stromal tumor) and PDGFRA (gastrointestinal stromal tumor) activation loop mutations in a phase 1 clinical study.