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Asciminib
- ABL001
- Optical Purity: 100% e.e.
- Soluble in 0.1N HCl(aq), DMSO and EtOH
- MF: C20H18ClF2N5O3
- MW: 449.84
Description
Asciminib is a potent and selective allosteric BCR-ABL1 inhibitor with an IC50 value of 0.5 nM (caliper assay). Moreover, Asciminib is the first-in-class STAMP (Specifically Targeting the ABL Myristoyl Pocket) inhibitor. In vivo, the combination of ABL001 and Nilotinib (Axon 1396) led to complete disease control and eradicated CML xenograft tumours without recurrence after the cessation of treatment.
More Information
| Parent CAS No. | 1492952-76-7 |
|---|---|
| Chemical Name | (R)-N-(4-(Chlorodifluoromethoxy)phenyl)-6-(3-hydroxypyrrolidin-1-yl)-5-(1H-pyrazol-5-yl)nicotinamide |
| SMILES | C1(OC(F)(F)Cl)C=CC(NC(=O)C2C=C(C3NN=CC=3)C(N3C[C@H](O)CC3)=NC=2)=CC=1 |&1:23,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C20H18ClF2N5O3/c21-20(22,23)31-15-3-1-13(2-4-15)26-19(30)12-9-16(17-5-7-25-27-17)18(24-10-12)28-8-6-14(29)11-28/h1-5,7,9-10,14,29H,6,8,11H2,(H,25,27)(H,26,30)/t14-/m1/s1 |
| InChiKey | VOVZXURTCKPRDQ-CQSZACIVSA-N |
| CID | 72165228 |
| Short Description | Bcr-Abl inhibitor |
References
- AA Wylie et al. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1. Nature. 2017 Mar 30;543(7647):733-737.
- J Schoepfer et al. Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1. J Med Chem. 2018 Sep 27;61(18):8120-8135.
- AE Eskazan et al. Asciminib in chronic myeloid leukemia: many questions still remain to be answered. Blood Cancer J. 2021 Apr 29;11(4):81.
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