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AP23464 and PF-562771 (AP23848) potently and selectively target activation-loop mutants of Kit in vitro and in vivo and could have therapeutic potential against D816V-expressing malignancies. Src/Abl inhibitors are compatible with imatinib and suggest that combined Abl inhibitor therapy is a feasible treatment strategy for patients with CML.
| Molecular Weight | 531.63 |
| Formula | C30H38N5O2P |
| CAS Number | 834894-21-2 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Src-bcr-Abl Products |
|---|
| AP24534
Ponatinib (AP24534) is a novel potent, orally available small molecule multitargeted kinase inhibitor of BCR-ABL, PDGFRα, c-Src, c-Kit, FGFR and VEGFR. |
| Saracatinib
Saracatinib (AZD0530) is an orally active small molecule Src inhibitor. |
| Bosutinib
Bosutinib (SKI-606) is a novel Bcr-Abl inhibitor with IC50 values of 0.1 to 0.3 umol/L. |
| Dasatinib
Dasatinib (BMS-354825) is a small molecule inhibitor of both the SRC and BCR/ABL tyrosine kinases, with IC50's for the isolated kinases of 0.55 and 3.0 nM, respectively. |
| DCC-2036
DCC-2036 is an ABL inhibitor with IC50 of 0.8 and 2 nM for u-ABL1native and p-ABL1native, respectively. |
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