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Avapritinib

SKU: orb1302083

Description

Avapritinib

Research Area

Product Categories/Products/Small Molecules,Tyrosine Kinase/Adaptors|||Angiogenesis

Images & Validation

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Avapritinib

Key Properties

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CAS Number1703793-34-3
MW498.56
Purity99.70%
FormulaC26H27FN10
SMILESCn1cc(cn1)-c1cc2c(ncnn2c1)N1CCN(CC1)c1ncc(cn1)[C@@](C)(N)c1ccc(F)cc1

Bioactivity

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Target IC50
c-Kit (D816V):0.27 nM|KIT D816 (human HMC1.2 cells):4 nM|KIT D816 (mouse P815):22 nM|ABCG2:0.2 μM (EC50, ATPase activity)|PDGFRα (D842V):0.24 nM|ABCB1:5 μM (EC50, ATPase activity)
In Vivo
METHODS: After a 21-day latency period post-injection, mice were orally administered Avapritinib (BLU-285) once daily at a dose of 10 mg/kg or 30 mg/kg until day 45. The efficacy of Avapritinib (BLU-285) in KIT exon 17 mutant CBF-AML was evaluated using the Kasumi-1 luc+ AML NOG SCID mouse femoral injection model. RESULTS Both doses (10 or 30 mg/kg, oral, once daily) of Avapritinib (BLU-285) significantly reduced disease burden throughout the study. Avapritinib (BLU-285) at 10 or 30 mg/kg resulted in tumor regression in all animals.
In Vitro
Avapritinib (BLU-285) has demonstrated biochemical in vitro activity against the KIT exon 17 mutant enzyme, KIT D816V, with an IC50 value of 0.27 nM; the cellular activity of BLU-285 on the KIT D816 mutant was measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2 and the P815 mouse mastocytoma cell line, with IC50 values ​​of 4 and 22 nM, respectively.
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.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Compound Identifiers

PubChem CID
118023034 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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1 mg
$ 180.00
5 mg
$ 300.00
1 ml x 10 mm (in DMSO)
$ 320.00
10 mg
$ 430.00
25 mg
$ 650.00
50 mg
$ 890.00
100 mg
$ 1,180.00
500 mg
$ 2,280.00
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