| Chemical Properties | Back Directory | [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| |
| Hazard Information | Back Directory | [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 |
|
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|