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CAS No. 1703793-34-3
Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).
Selleck's Avapritinib (BLU-285) has been cited by 5 publications
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|Description||Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibits PDGFRα D842V mutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogous Kit (c-Kit) mutation, D816V in Kit (c-Kit) Exon 17 (IC50 = 0.5 nM).|
BLU-285 is a selective oral inhibitor that targets KIT Exon 17 and PDGFRα D842 activation loop mutants. Cellular assays measuring inhibition of KIT mutant autophosphorylation confirm the activity of BLU-285 against the KIT D816 mutants D816V (HMC1.2 cells, IC50 = 3 nM) and D816Y (P815 cells, IC50 = 22 nM) as well as other KIT Exon 17 mutants such as N822K (Kasumi cells, IC50 = 40 nM) found in treatment-refractory GIST.
|In vivo||In vivo, BLU-285 is a well-tolerated, orally bioavailable agent that achieves dose dependent tumor growth inhibition in a D816Y-driven xenograft model. A PK-PD-efficacy relationship with BLU-285 has been established demonstrating that tumor regression results from >90% target suppression and is observed with 30 mg/kg once daily dosing. With potent activity against PDGFRα D842V and KIT Exon 17 mutants, BLU-285 targets previously unaddressed genomic drivers of disease and provides promise for the treatment of PDGFRα D842V-driven GIST(gastrointestinal stromal tumor) or SM(systemic mastocytosis), where more than 90% of patients carry the KIT D816V mutation. Besides single agent activity, the highly selective BLU-285 offers an opportunity for combination with other agents in GIST to cover the entirety of KIT primary and resistance mutants.|
|In vitro||DMSO||66 mg/mL (132.38 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04695431||Enrolling by invitation||--||Advanced Systemic Mastocytosis|Aggressive Systemic Mastocytosis|Systemic Mastocytosis With an Associated Hematological Neoplasm|Mast Cell Leukemia||Blueprint Medicines Corporation|Analysis Group Inc.||December 2 2020||--|
|NCT03731260||Recruiting||Drug: Avapritinib|Drug: Placebo||Indolent Systemic Mastocytosis||Blueprint Medicines Corporation||April 16 2019||Phase 2|
|NCT03580655||Active not recruiting||Drug: Avapritinib||Advanced Systemic Mastocytosis|Aggressive Systemic Mastocytosis|Systemic Mastocytosis With an Associated Hematologic Neoplasm|Mast Cell Leukemia||Blueprint Medicines Corporation||November 21 2018||Phase 2|
|NCT03465722||Active not recruiting||Drug: avapritinib|Drug: regorafenib||GIST||Blueprint Medicines Corporation||March 26 2018||Phase 3|
|NCT02561988||Active not recruiting||Drug: Avapritinib||Aggressive Systemic Mastocytosis|Systemic Mastocytosis-associated Hematologic Non-mast Cell Disease|Mast Cell Leukemia|Relapsed or Refractory Myeloid Malignancies||Blueprint Medicines Corporation||March 10 2016||Phase 1|
|NCT02508532||Active not recruiting||Drug: Avapritinib||Gastrointestinal Stromal Tumors (GIST)|Other Relapsed or Refractory Solid Tumors||Blueprint Medicines Corporation||August 2015||Phase 1|
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