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Avapritinib

SKU: orb1302083

Description

Avapritinib

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

Key Properties

CAS Number1703793-34-3
MW498.56
Purity99.70%
FormulaC26H27FN10
SMILESCn1cc(cn1)-c1cc2c(ncnn2c1)N1CCN(CC1)c1ncc(cn1)[C@@](C)(N)c1ccc(F)cc1
TargetPDGFR,c-Kit
SolubilityH2O:Insoluble;10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (8.02 mM);Ethanol:3 mg/mL (6.02 mM);DMSO:120 mg/mL (240.69 mM)

Bioactivity

Target IC50
c-Kit (D816V):0.27 nM|KIT D816 (human HMC1. 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- mL was evaluated usin the Kasumi-1 luc+ mL 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 throughou 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 agains the KIT exon 17 mutant enzyme, KIT D816V, with an IC50 value of 0.27 nM the cellular activity of BLU-285 o the KIT D816 mutant was measured by autophosphorylation in the human mast cell leukemia cell line HMC1.2 an the P815 mouse mastocytoma cell line, with IC50 Values ​​of 4 and 22 nM, respectively
Animal Research
A Kasumi-1 luc+ mL NOG SCID mouse femoral injection model is used to asses 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

Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
DisclaimerFor research use only

Alternative Names

BLU 285, BLU285, BLU-285, Avapritinib, cKit, c-Kit, CD117, inhibit, PDGFR, Platelet-derived growth factor receptor, Inhibitor, PDGFRα, SCFR

Similar Products

  • Avapritinib [orb1225956]

    >98% (HPLC)

    1703793-34-3

    498.6

    C26H27FN10

    10 mg, 25 mg, 50 mg, 100 mg, 5 mg, 1 g, 500 mg
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Key Properties

No computed properties available.

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Avapritinib (orb1302083)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,040.00
5 mg
¥ 1,560.00
10 mg
¥ 2,210.00
1 ml x 10 mM (in DMSO)
¥ 2,990.00
25 mg
¥ 3,900.00
50 mg
¥ 5,590.00
100 mg
¥ 9,100.00
200 mg
¥ 12,480.00
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