MK256 is a novel CDK8 inhibitor with potent antitumor activity in AML through downregulation of the STAT pathway. MK256 induced differentiation and maturation. Treatment of MK256 inhibited proliferation of AML cell lines. MK256 not only downregulated phosphorylated STAT1(S727) and STAT5(S726), but also lowered mRNA expressions of MCL-1 and CCL2 in AML cell lines. Efficacy of MK256 was shown in MOLM-14 xenograft models, and the inhibitory effect on phosphorylated STAT1(S727) and STAT5(S726) with treatment of MK256 was observed in vivo. Pharmacologic dynamics study of MK256 in MOLM-14 xenograft models showed dose-dependent inhibition of the STAT pathway. Both in vitro and in vivo studies suggested that MK256 could effectively downregulate the STAT pathway.
MedKoo Cat#: 130252
Name: MK256
CAS#: 2271348-04-8 (free acid)
Chemical Formula: C14H9BrN2O2
Exact Mass: 315.9847
Molecular Weight: 317.14
Elemental Analysis: C, 53.02; H, 2.86; Br, 25.20; N, 8.83; O, 10.09
The following data is based on the product molecular weight 317.14 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
