1. Protein Tyrosine Kinase/RTK
  2. c-Kit
  3. Avapritinib

Avapritinib (Synonyms: BLU-285)

Cat. No.: HY-101561 Purity: >98.0%
Handling Instructions

Avapritinib is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.

For research use only. We do not sell to patients.

Avapritinib Chemical Structure

Avapritinib Chemical Structure

CAS No. : 1703793-34-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 274 In-stock
Estimated Time of Arrival: December 31
1 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 390 In-stock
Estimated Time of Arrival: December 31
25 mg USD 690 In-stock
Estimated Time of Arrival: December 31
50 mg USD 990 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Avapritinib is a potent and selective exon 17 mutant KIT kinase inhibitor with IC50 of 0.27 nM for KIT D816V.

IC50 & Target

IC50: 0.27 nM (KIT D816V)[1]

In Vitro

Avapritinib (BLU-285) has demonstrated biochemical in vitro activity on the KIT exon 17 mutant enzyme, KIT D816V (IC50=0.27 nM). 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, a t(8;21)-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

In vivo Avapritinib (BLU-285) is well tolerated and has demonstrated dose dependent antitumor efficacy. Complete tumor growth inhibition and ≥75% KIT kinase inhibition is observed with 10 mg/kg once daily, oral dosing of Avapritinib in the aggressive KIT exon 17 mutant driven P815 mastocytoma model grown as a solid tumor allograft as well as in a disseminated model of disease. Disease burden, measured by whole body luciferase imaging (photons/second/mm2), increases 86-fold in the vehicle control animals over the 24 day dosing period with widespread disease detectable in both femurs, the pelvis and circulating in peripheral blood. Avapritinib at both doses (10 or 30 mg/kg orally, once daily) results in a marked reduction of disease burden throughout the study. Avapritinib at either 10 or 30 mg/kg results in tumor regression in all animals with disease abrogation indistinguishable from background signal measurements in several animals by the end of study. Avapritinib is also well tolerated in this in vivo model and has no adverse effects on body weight at either dose[1].

Clinical Trial
Molecular Weight

498.56

Formula

C₂₆H₂₇FN₁₀

CAS No.

1703793-34-3

SMILES

CN1N=CC(C2=CN3C(C(N4CCN(C5=NC=C([[email protected]@](C)(N)C6=CC=C(F)C=C6)C=N5)CC4)=NC=N3)=C2)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 83.33 mg/mL (167.14 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0058 mL 10.0289 mL 20.0578 mL
5 mM 0.4012 mL 2.0058 mL 4.0116 mL
10 mM 0.2006 mL 1.0029 mL 2.0058 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.01 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Mice[1]
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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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