Free shipping on all orders over $ 500
Asciminib (ABL001) selectively inhibited the growth of CML and Ph+ ALL cells with potencies ranging from 1-10nM range. Asciminib was tested for activity against clinically observed mutations and found to be active in the low nM range. In the KCL-22 mouse xenograft model, Asciminib displayed potent anti-tumor activity with complete tumor regression observed and a clear dose-dependent correlation with pSTAT5 inhibition. The oral bioavailability of ABL001 in mouse and rat are 35% and 27% respectively when dosed at 30 mg/kg p.o. While in dogs the oral BA of ABL001 is 111% (15 mg/kg, p.o).
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Molecular Weight | 449.84 |
| Formula | C20H18ClF2N5O3 |
| CAS Number | 1492952-76-7 |
| Purity | >99% |
| Solubility | DMSO ≥ 40 mg/mL |
| Storage | at -20°C |
[1] Wylie AA, et al. Nature. The allosteric inhibitor ABL001 enables dual targeting of BCR-ABL1.
| Related Src-bcr-Abl Products |
|---|
| 1NM-PP1
1NM-PP1 is a cell-permeable and potent Src family kinases inhibitor with IC50 values of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. |
| TL02-59
TL02-59 is a selective, orally active Src-family kinase Fgr inhibitor with IC50 of 0.03 nM, it also inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. |
| CZC-8004
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase. |
| Flumatinib mesylate
Flumatinib mesylate is a selective inhibitor of BCR-ABL/PDGFR/c-Kit with IC50s of 1.2 nM, 307.6 nM and 2662 nM, respectively. |
| TG-100572 hydrochloride
TG-100572 hydrochloride is a potent and selective multi-targeted VEGFR2/Src kinase inhibitor. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.
