Description
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.
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.
Alternate Name/Synonyms: 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
Formulation:
CAS Number: 1703793-34-3
Structure Available?: TRUE
Peptide sequence:
Salt Form: FALSE
Molecular Formula: C₂₆H₂₇FN₁₀
Molecular Weight: 498.56
Cell-Permeable?: FALSE
Purity: >98%
Solubilities: ~ 66 mg/ml in DMSO, ~ 3 mg/ml in Ethanol
Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Country of Origin: USA
Tag Line: An inhibitor of oncogenic KIT and PDGFRA mutations
MDL Number: MFCD31544325
PubChem CID: 118023034
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
Additional Information
Storage Condition: |
-20ºC |
Shipping Condition: |
RT |
Shelf Life: |
36 months |