PD 0332991 HCl (Palbociclib)

Catalog No. A10701

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。

Product Citations

Hiroki Ozawa, .et al. Targeting AURKA in treatment of peritoneal tumor dissemination in gastrointestinal cancer, Transl Oncol, 2022, Feb;16:101307 PMID: 34902741
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

Technical details

Catalog Num	A10701
M. Wt	447.5
Formula	C24H29N7O2.HCl
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	827022-32-2
Synonyms
SMILES	CC1=C(C(=O)N(C2=NC(=NC=C12)NC3=NC=C(C=C3)N4CCNCC4)C5CCCC5)C(=O)C.Cl

Biological Activity

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

Solubility *

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.

Preparing Stock Solutions

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.