GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

5-​Pyrimidinemethanamin​e, α-​(4-​fluorophenyl)​-​α-​methyl-​2-​[4-​[6-​(1-​methyl-​1H-​pyrazol-​4-​yl)​pyrrolo[2,​1-​f]​[1,​2,​4]​triazin-​4-​yl]​-​1-​piperazinyl]​-​, (αS)​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Avapritinib (BLU-285) is a small molecule kinase inhibitor that potently inhibitsPDGFRα D842Vmutant activity in vitro (IC50 = 0.5 nM) and PDGFRα D842V autophosphorylation in the cellular setting (IC50 = 30 nM); also a potent inhibitor of the analogousKit
In vitro

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.
Cell Data

cell lines：Wild-type and mLST8 deficient MEFs

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Synonyms

5-​Pyrimidinemethanamin​e, α-​(4-​fluorophenyl)​-​α-​methyl-​2-​[4-​[6-​(1-​methyl-​1H-​pyrazol-​4-​yl)​pyrrolo[2, ​1-​f]​[1, ​2, ​4]​triazin-​4-​yl]​-​1-​piperazinyl]​-​, (αS)​-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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 K

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Platelet-derived growth factor receptor alpha inhibitor

Product Properties

• ALogP: 1.9

Names and Identifiers

• Isomeric SMILES: C[C@](C1=CC=C(C=C1)F)(C2=CN=C(N=C2)N3CCN(CC3)C4=NC=NN5C4=CC(=C5)C6=CN(N=C6)C)N
• Molecular Weight: 498.56
• Reaxy-Rn: 28010820
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=28010820&ln=

Associated Targets(Human)

KIT Tclin Mast/stem cell growth factor receptor Kit (0 Activities)

Discover Target: KIT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 30 mg/mL (118.92 mM); Water: Insoluble; Ethanol: Insoluble