For research use only. Not for therapeutic Use.
Elenestinib (BLU-263) is a potent and orally active tyrosine kinase inhibitor. Elenestinib has the potential for the research of systemic mastocytosis (SM). Elenestinib inhibits KIT D816V with an IC50 value of 0.2 nM[1][2].
| CAS Number | 2505078-08-8 |
| Synonyms | 2-[4-[4-[4-[5-[(1S)-1-amino-1-(4-fluorophenyl)ethyl]pyrimidin-2-yl]piperazin-1-yl]pyrrolo[2,1-f][1,2,4]triazin-6-yl]pyrazol-1-yl]ethanol |
| Molecular Formula | C27H29FN10O |
| Purity | ≥95% |
| InChI | InChI=1S/C27H29FN10O/c1-27(29,21-2-4-23(28)5-3-21)22-14-30-26(31-15-22)36-8-6-35(7-9-36)25-24-12-19(17-38(24)34-18-32-25)20-13-33-37(16-20)10-11-39/h2-5,12-18,39H,6-11,29H2,1H3/t27-/m0/s1 |
| InChIKey | IPMARPMXSFFZFG-MHZLTWQESA-N |
| SMILES | CC(C1=CC=C(C=C1)F)(C2=CN=C(N=C2)N3CCN(CC3)C4=NC=NN5C4=CC(=C5)C6=CN(N=C6)CCO)N |
| Reference | [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]. Mariana Castells, et al. A Phase 2/3 Study of BLU-263 in Patients with Indolent Systemic Mastocytosis or Monoclonal Mast Cell Activation Syndrome. Allergy and Clinical Immunology. 2022, 149 (2). |
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