CX 6258 hydrochloride hydrate
Data Sheet
For research use only. Not for human use.
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| CAS No. | 1353858-99-7 | Cat. No. | BCP19056 |
| Name | CX 6258 hydrochloride hydrate | ||
| Synonyms | CX-6258 hydrochloride hydrate;CX6258 hydrochloride hydrate; | ||
| SMILES | |||
| Chemical Name | |||
| Formula | C26H24ClN3O3.HCl.H2O | M. Wt | 516.42 |
| Purity | 98% | Storage | Store at 4-8°C |
| Description | in vitro: CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM). CX-6258 showed robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. In mechanistic cellular assays with MV-4-11 human AML cells, (13) caused dose-dependent inhibition of the phosphorylation of 2 pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively[1]. Pim-1 inhibition using the small molecule inhibitor CX-6258 (12 mM, 3 h) diminishes endogenous NKX3.1 steady state levels in 22RV1 and LNCaP cells. CX-6258 treatment (12 mM, 3 h) treatment diminished steady-state levels of ectopic NKX3.1 in PC3 cells. CX-6258 treatment resulted in a significant reduction in NKX3.1 half | ||
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