生物活性
PD 0332991 HCl (Palbociclib)是一种高度选择性的CDK4/6抑制剂,它对CDK1/2/5,EGFR,FGFR,PDGFR,InsR等没有抑制活性,具有潜在的抗肿瘤活性。
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 |
化学数据
目录号 | A10701 |
作用机制 | Inhibitor (抑制剂) |
M. Wt | 447.5 |
Formula | C24H29N7O2.HCl |
Purity | >99% |
Storage | Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for36 months. In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
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 |
溶解度
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. |
储备液配制
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.