Elenestinib (phosphate)

Elenestinib (BLU-263) phosphate is an orally active inhibitor of Tyrosine kinase with an IC50 of 0.2 nM for KIT D816V. Elenestinib phosphate minimally penetrates the blood-brain barrier. Elenestinib phosphate can be used in the study of systemic mastocytosis[1][2].

Product Specifications

CAS Number

[2832013-93-9]

Product Name Alternative

BLU-263 (phosphate)

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-phosphate.html

Solubility

10 mM in DMSO

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.OP(O)(O)=O

Molecular Formula

C27H32FN10O5P

Molecular Weight

626.58

References & Citations

[1]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.|[2]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.