MedChemExpress LLC (MCE)

MedChemExpress - Model Elenestinib - 2505078-08-8

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].

Elenestinib

MCE China：Elenestinib

Brand：MedChemExpress (MCE)

Cat. No.HY-152839

CAS：2505078-08-8

Synonyms：BLU-263

Purity：98.82%

Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：Activity of Elenestinib against closely related kinases relative to KIT activity in cells (IC50 (nM))[3] PDGFRα PDGFRß CSF1R FLT3 KDR 21 6 161 345 >1000

In Vivo：Elenestinib (30 mg/kg, oral gavage, a single dose for 30 h) demonstrates brain penetration with brain to plasma ratio of 0.18 in rats[3].

IC50 & Target：IC50: 0.2 nM (KIT D816V)[1] In Vitro Activity of Elenestinib against closely related kinases relative to KIT activity in cells (IC50 (nM))[3] PDGFRα PDGFRß CSF1R FLT3 KDR

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.

[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).

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