Asciminib hydrochloride
- Product Name
- Asciminib hydrochloride
- CAS No.
- 2119669-71-3
- Chemical Name
- Asciminib hydrochloride
- Synonyms
- Asciminib HCl;Asciminib hydrochloride;Asciminib hydrochloride （ABL-001）;N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1H-pyrazol-5-yl)nicotinamide hydrochloride;(R)-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1H-pyrazol-3-yl)nicotinamide hydrochloride;(R)-N-(4-(Chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1H-pyrazol-5-yl)nicotinamide hydrochloride;(R)-N-(4-(Chloro-difluoromethoxy)phenyl)-6-(3-hydroxy-pyrrolidin-1-yl)-5-(1H-pyrazol-3-yl)-pyridin-3-carboxamide HCl
- CBNumber
- CB94848199
- Molecular Formula
- C20H18ClF2N5O3. HCl
- Formula Weight
- 486.3
- MOL File
- 2119669-71-3.mol
Asciminib hydrochloride Property
- storage temp.
- 4°C, away from moisture
- form
- Solid
- color
- White to off-white
- InChIKey
- HGCOOPLEWPBLOY-XOIICWPPNA-N
- SMILES
- C(C1C=NC(N2C[C@H](O)CC2)=C(C2=NNC=C2)C=1)(=O)NC1C=CC(OC(F)(F)Cl)=CC=1.Cl |&1:7,r|
Asciminib hydrochloride Chemical Properties,Usage,Production
Description
Asciminib Hydrochloride is the hydrochloride form of asciminib, an orally bioavailable variant Bcr-Abl1 tyrosine kinase inhibitor with antitumour activity. Upon administration, aximinib targets and binds to the myristoyl pocket of the Bcr-Abl1 fusion protein that is distinct from the ATP-binding domain, thereby inhibiting the activity of wild-type Bcr-Abl and certain mutants, including the T315I mutation. This binding inhibits Bcr-Abl1-mediated proliferation and enhances apoptosis in Philadelphia chromosome-positive (Ph+) haematological malignancies.The Bcr-Abl1 fusion protein tyrosine kinase is an aberrant enzyme produced by Philadelphia chromosome-containing leukaemia cells.
Uses
Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM[1].
Indications
Asciminib hydrochloride is approved for the treatment of adult patients with chronic myeloid leukaemia (CML) who are in the chronic phase and are Philadelphia chromosome positive. This includes:
Patients who have been treated with at least two tyrosine kinase inhibitors;
Patients with CML who have the T315I mutation;
Newly diagnosed CML patients
in vivo
Single doses of 7.5, 15 and 30 mg/kg Asciminib, administered to mice bearing KCL- 22 xenografts, inhibits pSTAT5 (Tyr694), which return to baseline at 10, 12 and 16-20 h after administration of the dose, respectively. In mice implanted with KCL-22 tumors, the minimum dose of Asciminib required for complete regression is 7.5 mg/kg twice a day (BID) or 30 mg/kg once a day (QD), and is tolerated at doses up to 250 mg/kg BID[1].
References
[1] Wylie AA, et al. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1. Nature. 2017 Mar 30;543(7647):733-737. DOI:10.1038/nature21702
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