Palbociclib (PD0332991) Isethionate

SKU: orb1223927

描述

Palbociclib (PD0332991) Isethionate is a highly selective inhibitor of CDK4/6 with IC50 of 11 nM/16 nM. It shows no activity against CDK1/2/5, EGFR, FGFR, PDGFR, InsR, etc. Phase 3.

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	827022-33-3
MW	573.66
纯度	>98% (HPLC)
分子式	C₂₄H₂₉N₇O₂·C₂H₆O₄S
SMILES	OCCS(O)(=O)=O.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	Water: 50 mg/mL warmed (87.15 mM)

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

相似产品

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Palbociclib Isethionate [orb1300947]
纯度：
99.85% (May vary between batches)
CAS 号：
827022-33-3
MW:
573.66
分子式：
C₂₄H₂₉N₇O₂·C₂H₆O₄S
可选规格： 5 mg, 10 mg, 1 ml x 10 mM (in DMSO)

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：	99.85% (May vary between batches)
CAS 号：	827022-33-3
MW:	573.66
分子式：	C₂₄H₂₉N₇O₂·C₂H₆O₄S