Palbociclib hydrochloride

SKU: orb1223928

Description

A potent and selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM; no inhibition for CDK2A (IC50>5 uM); inhibits MDA-MB453 cells with IC50 of 0.16 uM; shows antiproliferative effect against retinoblastoma (Rb)-positive tumor cells in vitro and reduces the phospho-Ser780/Ser795 on the Rb protein; orally bioavailable.Breast Cancer Approved.

Research Area

Pharmacology & Drug Discovery

Images & Validation

−

Key Properties

−

CAS Number	827022-32-2
MW	483.9937
Purity	>98% (HPLC)
Formula	C₂₄H₃₀ClN₇O₂
SMILES	Cl.CC(=O)C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N3CCNCC3)N=C2N(C2CCCC2)C1=O
Target	CDK
Solubility	DMSO: 6 mg/mL (Need ultrasonic or warming)

Bioactivity

−

In Vivo

Animal model: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted). Dosage: 75, 150 mg/kg, daily for 14 days. Administration: Oral adminstration. Result: Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days. Animal model: Tumor-free female FVB mice. Dosage: 90 mg/kg (diluted in 50 nM sodium D-lactate), daily for 12 days. Administration: Oral adminstration. Result: Reduced total thymic mass and immature CD4+ and CD8+ double-positive thymocytes, and increased the fractions of CD4+ and CD8+ single-positive thymocytes. Animal model: Genetically engineered mosaic mouse model of liver cancer (Myc; p53-sgRNA). Dosage: 100 mg/kg, daily for 1 week. Administration: Oral adminstration. Result: Decreased the luminescence signal in liver and delayed tumour growth.

Storage & Handling

−

Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

PD-0332991 hydrochloride | PD0332991 hydrochloride | PD 0332991 hydrochloride

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at support@biorbyt.com.

Quick Database Links

Gene Symbol

CDK

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols