Biological Activity
PHA-848125 (Milciclib) is an orally bioavailable inhibitor of CDKs and TRKA with potential antineoplastic activity.
Targets
Target | Value |
---|---|
CDK2/CyclinA | IC50: 45nM |
TrkA | IC50: 53nM |
CDK7/CyclinH | IC50: 150nM |
CDK4/CyclinD1 | IC50: 160nM |
CDK5/p35 | IC50: 265nM |
CDK2/CyclinE | IC50: 363nM |
CDK1/CyclinB | IC50: 398nM |
In vitro (25°C) | DMSO | 91 mg/mL (197.58 mM) | |
Water | Insoluble | ||
Ethanol | Insoluble | ||
In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W | 28 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 | 21.71 mL | 108.55 mL | 217.11 mL |
0.5 mM | 4.34 mL | 21.71 mL | 43.42 mL |
1 mM | 2.17 mL | 10.86 mL | 21.71 mL |
5 mM | 0.43 mL | 2.17 mL | 4.34 mL |
*The above data is based on the productmolecular weight 460.6 . 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 | A11047 |
---|---|
Actions | Inhibitor |
CAS No. | 802539-81-7 |
Formula | C25H32N8O |
M. Wt | 460.6 |
Purity | >98% |
Synonyms | Milciclib, PHA848125 |
SMILES | CC1(CC2=CN=C(N=C2C3=C1C(=NN3C)C(=O)NC)NC4=CC=C(C=C4)N5CCN(CC5)C)C |
Storage | Store lyophilized at -20ºC, keep desiccated. |
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