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Avapritinib

An inhibitor of oncogenic KIT and PDGFRA mutations
Catalog #: B2999
SKU-Size Size Price Qty
B2999-1 1 mg
$75.00
B2999-5 5 mg
$295.00
More Sizes Get Quote

Product Details

Alternate Name 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
Handling Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Storage Conditions -20ºC
Shipping Conditions RT
USAGE For Research Use Only! Not For Use in Humans.

Details

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.


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