Avapritinib

SKU: orb1302083

Description

Avapritinib (BLU-285) is a potent, oral inhibitor targeting mutant KIT (D816V) and PDGFRA (D842V) kinases with sub-nanomolar IC50 values. It also inhibits ABCB1 and ABCG2 transporters. This agent demonstrates antitumor efficacy in research models of systemic mastocytosis and gastrointestinal stromal tumors (GIST).

Research Area

Cardiovascular Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	1703793-34-3
MW	498.56
Purity	99.70%
Formula	C₂₆H₂₇FN₁₀
SMILES	Cn1cc(cn1)-c1cc2c(ncnn2c1)N1CCN(CC1)c1ncc(cn1)[C@@](C)(N)c1ccc(F)cc1
Target	PDGFR,c-Kit
Solubility	H2O: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

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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) Read more...
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. Read more...
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. Read more...
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. Read more...

Storage & Handling

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Storage	store 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.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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

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Compound Identifiers

PubChem CID

118023034 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	1703793-34-3
MW:	498.57
Formula:	C₂₆H₂₇FN₁₀

Avapritinib

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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