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) .