product name AMG 925
Description: AMG 925, also known as FLX925, is a potent, selective and orally bioavailable dual FLT3/CDK4 inhibitor with IC50 of 1 nM and 3 nM, respectively. AMG 925 inhibits cell growth (IC50 values of 19nM and 18nM, respectively) through inhibiting P-FLT3 and P-STAT5 and inducing apoptosis. AML tumor–bearing mice, administration of AMG 925 shows inhibition of P-STAT5 and P-RB as well as cell growth both in subcutaneous MOLM13 xenograft tumor model and systemic MOLM13-Luc xenograft tumor model.
References: Mol Cancer Ther. 2014 Apr;13(4):880-9.
471.55
Formula
C26H29N7O2
CAS No.
1401033-86-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 10 mM
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
2% hydroxypropyl methylcellulose+1% Tween 80: 30mg/mL
Synonyms
FLX925
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19421245
| In Vitro |
In vitro activity: AMG 925 inhibits cell growth (IC50 values of 19nM and 18nM, respectively) through inhibiting P-FLT3 and P-STAT5 and inducing apoptosis. FLT3 mutants cause resistance to the current FLT3 inhibitors. AMG 925 is reported to inhibit cell growth in AML cells with FLT3 mutants FLT3-D835Y and FLT3-D835V. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In AML tumor –bearing mice, administration of AMG 925 shows inhibition of P-STAT5 and P-RB as well as cell growth both in subcutaneous MOLM13 xenograft tumor model and systemic MOLM13-Luc xenograft tumor model. AMG 925 is also reported to have antitumor activity in a dose-dependent manner in theRB-positive Colo205 colon adenocarcinoma xenograft model. |
| Animal model | |
| Formulation & Dosage | |
| References | Mol Cancer Ther. 2014 Apr;13(4):880-9 |
