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Avapritinib

Avapritinib

€738.00

Excl. VAT

Item no.	HY-101561-100mg
Manufacturer	MedChem Express
CASRN	1703793-34-3
Amount	100 mg
Category	Oncology Neuroscience Neural Lineage Markers Inhibitors & Compound Libraries Small Molecules By Organ Colorectal Cancer Heart & Blood Cancer Microglia Markers
Type	Inhibitors
Specific against	other
Purity	99.94
Formula	C26H27FN10
Citations	[1]Evans EK, et al. A precision therapy against cancers driven by KIT/PDGFRA mutations. Sci Transl Med. 2017 Nov 1;9(414). pii: eaao1690. [2]Erica Evans, et al. Blu-285, a Potent and Selective Inhibitor for Hematologic Malignancies with KIT Exon 17 Mutations.Blood 2015 126:568. [3]Wu CP, et al. Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-MediatedMultidrug Resistance in Cancer Cell Lines. Mol Pharm. 2019 Jul 1;16(7):3040-3052.
Smiles	CN1N=CC(C2=CN3C(C(N4CCN(C5=NC=C([C@@](C)(N)C6=CC=C(F)C=C6)C=N5)CC4)=NC=N3)=C2)=C1
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	BLU-285
Available
Product Description	Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2[1][2].
StorageTemperature	-20°C, 3 years; 4°C, 2 years (Powder)
Shipping	Room Temperature
Manufacturers Applications	Cancer-Kinase/protease
Molecular Weight	498.56
Clinical Information	Launched
Solubility	DMSO : ≥ 83.33 mg/mL
Pathway	Protein Tyrosine Kinase/RTK
Manufacturers Product type	Reference compound

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HY-101561-100mg-safety-datasheet.pdf