- 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 | Warmed: 3 mg/mL (6.19 mM) | |
Water | 30 mg/mL (61.98 mM) | ||
Ethanol | Insoluble | ||
In vivo | Saline | 5 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 | 20.66 mL | 103.31 mL | 206.61 mL |
0.5 mM | 4.13 mL | 20.66 mL | 41.32 mL |
1 mM | 2.07 mL | 10.33 mL | 20.66 mL |
5 mM | 0.41 mL | 2.07 mL | 4.13 mL |
*The above data is based on the productmolecular weight 484.0. 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 |
CAS No. | 827022-32-2 |
Formula | C24H29N7O2.HCl |
M. Wt | 484.0 |
Purity | >98% |
SMILES | CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl |
Storage | Store lyophilized at -20ºC, keep desiccated. |
Datasheet
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