- Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
- Pirita Pekkonen, .et al. KSHV viral cyclin interferes with T-cell development and induces lymphoma through Cdk6 and Notch activation in vivo, Cell Cycle., 2014, Dec 1; 13(23): 3670-3684. PMID: 25483078
Biological Activity
PD 0332991 HCl is an orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity.
Targets
Target | Value |
---|---|
CDK4/CyclinD3 | IC50: 9nM |
CDK4/CyclinD1 | IC50: 11nM |
CDK6/CyclinD2 | IC50: 15nM |
CDK2/CyclinE2 | IC50: >10μM |
CDK2/CyclinA | IC50: >10μM |
CDK1/CyclinB | IC50: >10μM |
CDK5/p25 | IC50: >10μM |
EGFR | IC50: >10μM |
FGFR | IC50: >10μM |
PDGFR | IC50: >10μM |
Insulin Receptor | IC50: >10μM |
VEGFR | IC50: >10μM |
AMPK | IC50: >10μM |
Chk1 | IC50: >10μM |
CK1 | IC50: >10μM |
CK2 | IC50: >10μM |
c-Src | IC50: >10μM |
GSK-3β | IC50: >10μM |
MAPK2/ERK2 | IC50: >10μM |
MAPKAPK2 | IC50: >10μM |
PKB | IC50: >10μM |
PKC | IC50: >10μM |
PHK | IC50: >10μM |
SAPK2a | IC50: >10μM |
SAPK3 | IC50: >10μM |
SAPK4 | IC50: >10μM |
In vitro (25°C) | DMSO | 3 mg/mL (6.19 mM) | |
Water | 30 mg/mL (61.98 mM) | ||
Ethanol | <1 mg/mL (<1 mM) | ||
In vivo | Saline | 20 mg/mL | |
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.1 mM | 22.35 mL | 111.73 mL | 223.46 mL |
0.5 mM | 4.47 mL | 22.35 mL | 44.69 mL |
1 mM | 2.23 mL | 11.17 mL | 22.35 mL |
5 mM | 0.45 mL | 2.23 mL | 4.47 mL |
*The above data is based on the productmolecular weight 447.5 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Catalog Num | A10701 |
---|---|
Actions | Inhibitor |
M. Wt | 447.5 |
Formula | C24H29N7O2.HCl |
Solubility | DMSO |
Purity | >98% |
Storage | at -20°C 3 years Powder |
CAS No. | 827022-32-2 |
SMILES | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl |
Datasheet
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