Palbociclib hydrochloride

SKU: orb1223928

描述

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.

研究领域

Pharmacology & Drug Discovery

图片与验证

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关键属性

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CAS 号	827022-32-2
MW	483.9937
纯度	>98% (HPLC)
分子式	C₂₄H₃₀ClN₇O₂
SMILES	Cl.CC(=O)C1=C(C)C2=CN=C(NC3=NC=C(C=C3)N3CCNCC3)N=C2N(C2CCCC2)C1=O
靶点	CDK
溶解性	DMSO: 6 mg/mL (Need ultrasonic or warming)

生物活性

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体内

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.

体外

Cell Cycle Analysis Cell line: MDA-MB-453 cells. Concentration: 0-1 μM. Incubation time: 24 h. Result: Arrested MDA-MB-453 cells in G1.Cell Proliferation Assay Cell line: ER-positive as well as HER2-amplified breast cancer cell lines (MDA-MB-175, ZR-75-30, CAMA-1, etc. ) Concentration: 0-10 μM. Incubation time: 6 days. Result: Inhibited growth of luminal ER-positive as well as HER2-amplified breast cancer cell lines.

储存与操作

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储存	Storage temperature: -20°C. Stability: ≥ 2 years
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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PD-0332991 hydrochloride | PD0332991 hydrochloride | PD 0332991 hydrochloride

相似产品

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Palbociclib hydrochloride [orb1686464]
纯度：
99.89% (May vary between batches)
CAS 号：
571189-11-2
MW:
520.46
分子式：
C₂₄H₃₁Cl₂N₇O₂
可选规格： 100 mg, 250 mg, 1 g
Palbociclib monohydrochloride [orb1300948]
纯度：
>99.99% (May vary between batches)
CAS 号：
827022-32-2
MW:
483.99
分子式：
C₂₄H₂₉N₇O₂·HCl
可选规格： 5 mg, 2 mg, 10 mg
Verapamil HCl [orb1310060]
纯度：
>98%
CAS 号：
152-11-4
MW:
491.06
分子式：
C₂₇H₃₈N₂O₄ ∙ HCl
可选规格： 1 g, 5 g

质量保证

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常用数据库链接

基因符号

CDK

实验方案信息

查看更多实验方案

纯度：	99.89% (May vary between batches)
CAS 号：	571189-11-2
MW:	520.46
分子式：	C₂₄H₃₁Cl₂N₇O₂

纯度：	>99.99% (May vary between batches)
CAS 号：	827022-32-2
MW:	483.99
分子式：	C₂₄H₂₉N₇O₂·HCl

纯度：	>98%
CAS 号：	152-11-4
MW:	491.06
分子式：	C₂₇H₃₈N₂O₄ ∙ HCl