Palbociclib Isethionate

SKU: orb1300947

描述

Palbociclib Isethionate (PD 0332991 isethionate) is a potent and selective CDK4/6 inhibitor with IC50 values of 11 and 16 nM, respectively, and demonstrates high selectivity across kinases. It is widely used in cancer research, particularly for studying cell cycle arrest in breast cancer models, both in vitro and in vivo.

研究领域

Cell Biology, 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	99.85% (May vary between batches)
分子式	C₂₄H₂₉N₇O₂·C₂H₆O₄S
SMILES	OCCS(O)(=O)=O.CC(=O)c1c(C)c2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n(C2CCCC2)c1=O
靶点	CDK
溶解性	DMSO:40 mg/mL (69.73 mM);H2O:57.4 mg/mL (100.06 mM)

生物活性

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靶点 IC50	CDK4-CyclinD3:9 nM (cell free)\|CDK4-CyclinD1:11 nM (cell free)\|CDK6-CyclinD2:15 nM (cell free)\|DYRK1A:2000 nM\|MAPK:8000 nM
体内	Oral administration of PD 0332991 to mice bearing the Colo-205 human colon carcinoma produces marked tumor regression. Therapeutic doses of PD 0332991 cause elimination of phospho-Rb and the proliferative marker Ki-67 in tumor tissue and down-regulation of genes under the transcriptional control of E2F .
体外	Palbociclib is a highly specific inhibitor of Cdk4 (IC50, 0.011 micromol/L) and Cdk6 (IC50, 0.016 micromol/L). It is a potent antiproliferative agent against retinoblastoma (Rb)-positive tumor cells in vitro, inducing an exclusive G1 arrest, with a concomitant reduction of phospho-Ser780/Ser795 on the Rb protein . In all of the cell lines except KP-MRT-YM, Palbociclib inhibited cell proliferation >50% (IC50 values 0.01 to 0.6 μM), and induced G1-phase cell cycle arrest. The sensitivity of the MRT cell lines to Palbociclib was inversely correlated with p16 expression. KP-MRT-YM cells overexpress p16 and were resistant to the growth inhibitory effect of Palbociclib . Cell lines representing luminal estrogen receptor-positive (ER+) subtype (including those that are HER2 amplified) were most sensitive to growth inhibition by Palbociclib while nonluminal/basal subtypes were most resistant .
细胞研究	Cells were seeded at 2 × 10^4 per well in a 96-well Cytostar T plate and incubated overnight to allow cells to attach. Varying concentrations of PD 0332991 were added to the wells and incubated for 24 hours at 37°C. [14C]thymidine (0.1 μCi) was added to each well and incorporation of the radiolabel was allowed to proceed for 72 hours. Incorporated radioactivity was determined with a β plate counter .
动物研究	Mice (18–22 g) were randomized and then implanted s.c. with tumor fragments (～30 mg) into the region of the right axilla. Treatment was initiated when tumors reached 100 to 150 mg. PD 0332991 was given according to the schedule and dose indicated in the table and figure legends by gavage as a solution in sodium lactate buffer (50 mmol/L, pH 4.0) based on mean group body weight. In all experiments, there were 12 mice in the control group and 8 mice each in the treated groups. Additional details for each experiment are given in the table legends .

储存与操作

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储存	-20°C
有效期	12 months from date of receipt.
免责声明	For research use only

别名

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Inhibitor, inhibit, Palbociclib, Palbociclib (PD0332991) Isethionate, Palbociclib Isethionate, PD0332991, PD-0332991, PD 0332991, PD 0332991 isethionate, hepatocellular carcinoma, HER2, HCC, estrogen receptor, Cyclin dependent kinase, Breast cancer, CDK6/CyclinD2, CDK, CDK4/CyclinD1, CDK4/CyclinD3, cell cycle

相似产品

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Palbociclib (PD0332991) Isethionate [orb1223927]
纯度：
>98% (HPLC)
CAS 号：
827022-33-3
MW:
573.66
分子式：
C₂₄H₂₉N₇O₂·C₂H₆O₄S
可选规格： 5 mg, 50 mg, 500 mg, 1 g, 10 mg, 100 mg, 200 mg

质量保证

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化合物标识

PubChem CID

11478676 ↗

关键属性

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暂无计算属性。

实验方案信息

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纯度：	>98% (HPLC)
CAS 号：	827022-33-3
MW:	573.66
分子式：	C₂₄H₂₉N₇O₂·C₂H₆O₄S

Palbociclib Isethionate

描述

研究领域

图片与验证

关键属性

生物活性

储存与操作

别名

相似产品

Palbociclib (PD0332991) Isethionate [orb1223927]

质量保证

化合物标识

关键属性

实验方案信息

可选规格