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Asciminib

Asciminib

Product ID A724091
Cas No. 1492952-76-7
Purity ≥98%
Product Unit SizeCostQuantityStock
1 mg $77.20 In stock
5 mg $270.20 In stock
25 mg $771.80 In stock
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Quicklinks

  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Description
  • Product Info
  • Shipping and Storage
  • Downloads
  • References
  • Custom Order

Description

Asciminib is an orally bioavailable, allosteric Bcr-Abl1 tyrosine kinase inhibitor, with antineoplastic activity. Upon administration, asciminib targets and binds to the myristoyl pocket of the Bcr-Abl1 fusion protein at a location that is distinct from the ATP-binding domain, thereby inhibiting the activity of both wild-type Bcr-Abl and certain mutation forms, including the T315I mutation. This binding results in the inhibition of Bcr-Abl1-mediated proliferation and enhanced apoptosis of Philadelphia chromosome-positive (Ph+) hematological malignancies. The Bcr-Abl1 fusion protein tyrosine kinase is an abnormal enzyme produced by leukemia cells that contain the Philadelphia chromosome.
NCI Thesaurus (NCIt)

Product Info

Cas No.

1492952-76-7

Purity

≥98%

Formula

C20H18ClF2N5O3

Formula Wt.

449.84

IUPAC Name

N-[4-[chloro(difluoro)methoxy]phenyl]-6-[(3R)-3-hydroxypyrrolidin-1-yl]-5-(1H-pyrazol-5-yl)pyridine-3-carboxamide

Synonym

ABL001; ABL-001; Asciminib free base

Shipping and Storage

Store Temp

-20°C

Ship Temp

Ambient

Downloads

Info Sheet

A724091 Info Sheet PDF

References

Gleixner K, Filik Y, Berger D, et al. Asciminib and ponatinib exert synergistic anti-neoplastic effects on CML cells expressing BCR-ABL1T315I-compound mutations. Am J Cancer Res. 2021 Sep 15;11(9):4470-4484. PMID: 34659899

Rea D, Hughes T. Development of asciminib, a novel allosteric inhibitor of BCR-ABL1. Crit Rev Oncol Hematol. 2022 Mar;171:103580. PMID: 35021069

Oruganti B, Lindahl E, Yang J, et al. Allosteric enhancement of the BCR-Abl1 kinase inhibition activity of nilotinib by cobinding of asciminib. J Biol Chem. 2022 Aug;298(8):102238. PMID: 35809644

Lin H, Saputra F, Audira G, et al. Investigating potential cardiovascular toxicity of two anti-leukemia drugs of asciminib and ponatinib in zebrafish embryos. Int J Mol Sci. 2022 Oct 3;23(19):11711. PMID: 36233014

Custom Order

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