CONTACT US
Home > Inhibitors/Agonists> > BLU-945
2660250-10-0-BLU-945 BLU-945

BLU-945

For research use only. Not for therapeutic Use.

  • CAT Number: I044044
  • CAS Number: 2660250-10-0
  • Molecular Formula: C28H37FN6O3S
  • Molecular Weight: 556.70
  • Purity: ≥95%
Inquiry Now
Related Small Molecules: BIO-32546     (+)-JQ1 PA     Atrasentan hydrochloride    

BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC)[1][2][3].
BLU-945 has inhibitory activity against the EGFRm/T790M double and EGFRm/T790M/C797Striple mutants with IC50 value range from 1.2-4.4 nM[2].
BLU-945 (0- 10 mM, 4 h) inhibit EGFR phosphorylation in the EGFR L858R/T790M/C797S, and EGFR ex19del/T790M/C797S mutant cell lines[2].
BLU-945 (oral, 0-100 mg/kg; bid) demonstrates potent, robust EGFR pathway inhibition and anti-tumor activity in triple-mutant Osimertinib (HY-15772)-resistant Ba/F3 CDX and PDCX models[2].


Catalog Number I044044
CAS Number 2660250-10-0
Synonyms

N-[2-[(3S,4R)-3-fluoro-4-methoxypiperidin-1-yl]pyrimidin-4-yl]-8-[(2R,3S)-2-methyl-3-(methylsulfonylmethyl)azetidin-1-yl]-5-propan-2-ylisoquinolin-3-amine

Molecular Formula C28H37FN6O3S
Purity ≥95%
InChI InChI=1S/C28H37FN6O3S/c1-17(2)20-6-7-24(35-14-19(18(35)3)16-39(5,36)37)22-13-31-27(12-21(20)22)32-26-8-10-30-28(33-26)34-11-9-25(38-4)23(29)15-34/h6-8,10,12-13,17-19,23,25H,9,11,14-16H2,1-5H3,(H,30,31,32,33)/t18-,19-,23+,25-/m1/s1
InChIKey LIMFPAAAIVQRRD-BCGVJQADSA-N
SMILES CC1C(CN1C2=C3C=NC(=CC3=C(C=C2)C(C)C)NC4=NC(=NC=C4)N5CCC(C(C5)F)OC)CS(=O)(=O)C
Reference

[1]. John Emmerson Campbell, et al. Inhibitors of mutant forms of egfr. Patent WO2021133809A1.

[2]. Sun Min Lim, et al. BLU-945, a fourth-generation, potent and highly selective epidermal growth factor receptor tyrosine kinase inhibitor with intracranial activity, demonstrates robust in vivo anti-tumor activity in models of osimertinib-resistant non-small cell lung cancer.

[3]. Meredith S Eno, et al. Discovery of BLU-945, a Reversible, Potent, and Wild-Type-Sparing Next-Generation EGFR Mutant Inhibitor for Treatment-Resistant Non-Small-Cell Lung Cancer. J Med Chem. 2022 Jul 28;65(14):9662-9677.
 [Content Brief]

[4]. Elaine Shum. et al. A phase 1/2 study of BLU-945 in patients with common activating EGFRmutant non-small cell lung cancer (NSCLC) (SYMPHONY trial-in-progress)

Request a Quote