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1420477-60-6

1420477-60-6 structure
1420477-60-6 structure
  • Name: Acalabrutinib
  • Chemical Name: Acalabrutinib
  • CAS Number: 1420477-60-6
  • Molecular Formula: C26H23N7O2
  • Molecular Weight: 465.507
  • Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Btk
  • Create Date: 2018-03-20 08:00:00
  • Modify Date: 2024-01-08 14:35:41
  • Acalabrutinib is a novel, potent, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM in in vitro assay.
Name Acalabrutinib
Synonyms (S)-4-(8-amino-3-(1-but-2-ynoylpyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide
Benzamide, 4-[8-amino-3-[(2S)-1-(1-oxo-2-butyn-1-yl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl]-N-2-pyridinyl-
4-{8-Amino-3-[(2S)-1-(2-butynoyl)-2-pyrrolidinyl]imidazo[1,5-a]pyrazin-1-yl}-N-(2-pyridinyl)benzamide
ACP-196
UNII:I42748ELQW
Description Acalabrutinib is a novel, potent, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM in in vitro assay.
Related Catalog
Target

IC50: 3 nM (BTK in CD69 B cell)[2]

In Vitro Acalabrutinib inhibits tyrosine phosphorylation of downstream targets of ERK, IKB, and AKT, in the in vitro signaling assay on primary human CLL cells[2].
In Vivo In the human CLL NSG xenograft model, acalabrutinib demonstrates on-target effects including decreased phosphorylation of PLCγ2, ERK and significant inhibition of CLL cell proliferation. Acalabrutinib significantly decreases tumor burden in the spleen of the mice. In the TCL1 adoptive transfer model, acalabrutinib treatment decreases phosphorylation of BTK, PLCγ2 and S6. Most notably, acalabrutinib results in a significant increase in survival compared to mice receiving vehicle[1]. Acalabrutinib (100 mg twice per day) assessed for thrombus formation at injured arterioles of the mice, exhibits more selective for inhibiting BTK and has virtually no inhibition of platelet activity[2].
References

[1]. Herman SE, et al. The Bruton's tyrosine kinase (BTK) inhibitor acalabrutinib demonstrates potent on-target effects and efficacy in two mouse models of chronic lymphocytic leukemia. Clin Cancer Res. 2016 Nov 30

[2]. Wu J, et al. Acalabrutinib (ACP-196): a selective second-generation BTK inhibitor. J Hematol Oncol. 2016 Mar 9;9:21
Density 1.4±0.1 g/cm3
Molecular Formula C26H23N7O2
Molecular Weight 465.507
Exact Mass 465.191315
PSA 118.51000
LogP 0.77
Index of Refraction 1.715
Hazard Codes Xi

Chemsrc provides CAS#:1420477-60-6 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 1420477-60-6 | Chemsrc address: https://m.chemsrc.com/en/baike/1197460.html

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