Elenestinib
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].
Product Specifications
CAS Number
2505078-08-8
Product Name Alternative
BLU-263
UNSPSC
12352005
Target
C-Kit
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/elenestinib.html
Purity
98.68
Solubility
DMSO : 125 mg/mL (ultrasonic)
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
Molecular Formula
C27H29FN10O
Molecular Weight
528.58
References & Citations
[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.|[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) .
Shipping Conditions
Blue Ice
Storage Conditions
-20°C, 3 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 3
Available Sizes
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