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Background Information:
AMG 925 is a potent, selective, and orally available FLT3/CDK4 dual inhibitor with in vitro IC50 values of 2 nM and 3 nM, respectively. In acute myeloid leukemia (AML) cell lines MOLM13 and Mv4-11, AMG 925 inhibits cell growth (with Cellular IC50 values of 19nM and 18nM, respectively) through inhibiting P-FLT3 and P-STAT5 and inducing apoptosis. AMG 925 inhibited AML xenograft tumor growth by 96% to 99% without significant body weight loss. The antitumor activity of AMG 925 correlated with the inhibition of STAT5 and RB phosphorylation, the pharmacodynamic markers for inhibition of FLT3 and CDK4, respectively. In addition, it was also found to inhibit FLT3 mutants (e.g., D835Y) that are resistant to the current FLT3 inhibitors (e.g., AC220 and sorafenib) (ref 1.)
Reference:
1.K. Keegan et al, Preclinical evaluation of AMG 925, a FLT3/CDK4 dual kinase inhibitor for treating acute myeloid leukemia. Mol Cancer Ther. 2014 Apr;13(4):880-9.
2. ZH Li, et al, Discovery of AMG 925, a FLT3 and CDK4 Dual Kinase Inhibitor with Preferential Affinity for the Activated State of FLT3, J. Med Chem, March 18, 2014.
APIM050077: AMG-925
CAS No.: 1401033-86-0.
Molecular Formula: C26H29N7O2 ? 0.2H2O.
Molecular Weight: 475.2.
Purity: 99% (HPLC at 215 and 254 nm).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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