Palbociclib monohydrochloride

SKU: orb1300948

描述

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	827022-32-2
MW	483.99
纯度	>99.99% (May vary between batches)
分子式	C₂₄H₂₉N₇O₂·HCl
SMILES	Cl.CC(=O)c1c(C)c2cnc(Nc3ccc(cn3)N3CCNCC3)nc2n(C2CCCC2)c1=O
靶点	CDK
溶解性	DMSO:5 mg/mL (10.33 mM);H2O:20 mg/mL (41.32 mM)

生物活性

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靶点 IC50	CDK6-CyclinD2:15 nM (cell free)\|CDK4-CyclinD1:11 nM (cell free)\|CDK4-CyclinD3:9 nM (cell free)\|MAPK:8000 nM\|DYRK1A:2000 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	PD 0332991 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, PD 0332991 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 PD 0332991 was inversely correlated with p16 expression. KP-MRT-YM cells overexpress p16 and were resistant to the growth inhibitory effect of PD 0332991 . Cell lines representing luminal estrogen receptor-positive (ER+) subtype (including those that are HER2 amplified) were most sensitive to growth inhibition by PD 0332991 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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Cyclin dependent kinase, CDK, CDK6/CyclinD2, CDK4/CyclinD1, CDK4/CyclinD3, cell cycle, Breast cancer, PD0332991 Hydrochloride, PD-0332991 Hydrochloride, PD 0332991 hydrochloride, PD 0332991 Hydrochloride, PD 0332991 monohydrochloride, Palbociclib, Palbociclib (PD-0332991) HCl, Palbociclib hydrochloride, Palbociclib Hydrochloride, Palbociclib monohydrochloride, Palbociclib Monohydrochloride, inhibit, estrogen receptor, Inhibitor, HCC, HER2, hepatocellular carcinoma

质量保证

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化合物标识

PubChem CID

11431660 ↗

关键属性

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暂无计算属性。

实验方案信息

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Palbociclib monohydrochloride

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

质量保证

化合物标识

关键属性

实验方案信息

可选规格