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BLU-263

Chemical Structure : BLU-263

CAS No.: 2505078-08-8

BLU-263 (Elenestinib, BLU263)

Catalog No.: PC-20030Not For Human Use, Lab Use Only.

Elenestinib (BLU-263, BLU263) is a potent, selective, oral next-generation KIT D816V inhibitor with IC50 of 0.2 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Elenestinib (BLU-263, BLU263) is a potent, selective, oral next-generation KIT D816V inhibitor with IC50 of 0.2 nM.
BLU-263 has ELISA IC50 of 6 nM against HMC1.2 human mast cells (V560G/D816V).
BLU-263 exhibits limited central nervous system penetration, shows potential for systemic mastocytosis (SM).

Physicochemical Properties

M.Wt 528.60
Formula C27H29FN10O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-2-(4-(4-(4-(5-(1-amino-1-(4-fluorophenyl)ethyl)pyrimidin-2-yl)piperazin-1-yl)pyrrolo[2,1-f][1,2,4]triazin-6-yl)-1H-pyrazol-1-yl)ethan-1-ol

References

1. Dave N, et al. Safety and pharmacokinetics of BLU-263, a next-generation KIT inhibitor, in healthy volunteers[C]//Cancer Res (AACR Annual Meeting Abstracts). 2021, 122.

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