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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $80 | In Stock | |
5 mg | $197 | In Stock | |
10 mg | $322 | In Stock | |
25 mg | $547 | In Stock | |
50 mg | $788 | In Stock | |
100 mg | $1,080 | In Stock | |
500 mg | $2,180 | In Stock | |
1 mL x 10 mM (in DMSO) | $216 | In Stock |
Description | Avapritinib (BLU-285) is a dual inhibitor targeting the mutant KIT receptor (KIT D816V, IC50: 0.27 nM) and PDGFRα (PDGFRα D842V, IC50: 0.24 nM). |
Targets&IC50 | c-Kit (D816V):0.27 nM, PDGFRα (D842V):0.24 nM |
In vitro | Cellular activity of Avapritinib on KIT D816 mutants is measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2, and the P815 mouse mastocytoma cell line with IC50=4 and 22 nM, respectively. In Kasumi-1 cells, at positive AML cell line with a KIT exon 17 N822K mutation, Avapritinib potently inhibits KIT N822K mutant autophosphorylation (IC50: 40 nM), downstream signaling, as well as cellular proliferation (IC50: 75 nM)[1]. |
In vivo | BLU-285 (0.3-30 mg/kg) reduces tumor volume in a P815 KITD814Y mastocytoma allograft mouse model and a GIST patient-derived mouse xenograft model in a dose-dependent manner. Formulations containing BLU-285 have been used to treat KIT- and PDGFRα-driven malignancies. |
Animal Research | A Kasumi-1 luc+ AML NOG SCID mouse femoral injection model is used to assess the efficacy of Avapritinib (BLU-285) in KIT exon 17-mutated CBF-AML. Following a 21 day post-injection latency period, mice are dosed with Avapritinib orally, once daily at 10 mg/kg or 30 mg/kg through day 45. Control groups are treated with vehicle or Cytarabine administered 100 mg/kg i.p once weekly. |
Alias | BLU-285 |
Molecular Weight | 498.56 |
Formula | C26H27FN10 |
Cas No. | 1703793-34-3 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: Insoluble Ethanol: 3 mg/mL DMSO: 100 mg/mL (200.58 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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