2505078-08-8
Chemical Structure
Elenestinib
Synonym(s): BLU-263
- CAS No.: 2505078-08-8
- Formula:C27H29FN10O
- Molecular Weight:528.58
IUPAC Name: (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
InChIKey: IPMARPMXSFFZFG-MHZLTWQESA-N
SMILES: OCCN1C=C(C=N1)C2=CN3N=CN=C(N4CCN(C5=NC=C([C@@](N)(C6=CC=C(C=C6)F)C)C=N5)CC4)C3=C2
Biological Activity: Elenestinib (BLU-263) is an orally active inhibitor of Tyrosine kinase with an IC50 value of 6 nM for KIT D816V. Elenestinib minimally penetrates the blood-brain barrier. Elenestinib can be used in the study of systemic mastocytosis[1][2][3].
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Elenestinib | 98.68% | Elenestinib (BLU-263) is an orally active inhibitor of Tyrosine kinase with an IC50 value of 6 nM for KIT D816V. Elenestinib minimally penetrates the blood-brain barrier. Elenestinib can be used in the study of systemic mastocytosis. | ||||||||||||||||||||
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- [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.
- [2]. Chifotides HT, et al. SOHO State of the Art Update and Next Questions: Current and Emerging Therapies for Systemic Mastocytosis. Clin Lymphoma Myeloma Leuk. 2024 Jun 25:S2152-2650(24)00239-8. [Content Brief]
- [3]. Guarnieri A, et al. Bezuclastinib is a differentiated KIT inhibitor that exhibits unique selectivity to KIT A-loop mutations, minimal brain penetration, and favorable pharmacokinetic properties in preclinical models[C]//Cancer Research. 615 CHESTNUT ST, 17TH FLOOR, PHILADELPHIA, PA 19106-4404 USA: AMER ASSOC CANCER RESEARCH, 2022, 82(12).
Keywords
