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Palbociclib monohydrochloride

Palbociclib monohydrochloride PD 0332991 monohydrochloride

Palbociclib (PD 0332991) monohydrochloride 是高选择性的 CDK4/6 抑制剂，IC50 分别为 11 nM 和 16 nM。Palbociclib monohydrochloride 有潜力用于 ER 阳性和 HER2 阴性乳腺癌的研究。

货号：
TK0266
规格：

1mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	827022-32-2
生物活性	Palbociclib (PD 0332991) monohydrochloride is a highly selective CDK4/6 inhibitor with IC50s of 11 nM and 16 nM, respectively. Palbociclib monohydrochloride has the potential for ER-positive and HER2-negative breast cancer research.
分子式	C24H29N7O2.ClH
分子量	483.99
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	H2O : 50 mg/mL (103.31 mM; Need ultrasonic) DMSO : 5 mg/mL (10.33 mM; ultrasonic and warming and heat to 60°C)
体内研究	Palbociclib (PD 0332991) monohydrochloride exhibits significant antitumor efficacy against multiple human tumor xenograft models. In mice bearing Colo-205 colon carcinoma xenografts (p16 deleted), daily p.o. dosing for 14 days with Palbociclib (150 or 75 mg/kg) produces rapid tumor regressions and a corresponding tumor growth delay of ~50 days with >1 log of tumor cell kill at the highest dose tested. At 37.5 mg/kg, the tumor slowly regressed during treatment. Even at doses as low as 12.5 mg/kg, a 13-day growth delay is obtained indicating a 90% inhibition of tumor growth rate. Likewise, robust antitumor activity is seen in the MDA-MB-435 breast carcinoma (p16 deleted) where complete tumor stasis is apparent at 150 mg/kg and some cell kill is evident at the highest dose.
体外研究	The IC50 of Palbociclib (PD 0332991) for reduction of retinoblastoma (Rb) phosphorylation at Ser in MDA-MB-435 breast carcinoma cells is 66 nM. Palbociclib is equally effective at reducing Rb phosphorylation at Ser in this tumor with an IC50 of 63 nM, and similar effects on both Ser and Ser phosphorylation are obtained in the Colo-205 colon carcinoma. The MP-MRT-AN (AN), KP-MRT-RY (RY), G401, and KP-MRT-NS (NS) cell lines are effectively inhibited by Palbociclib (PD) in a concentration-dependent manner in a WST-8 assay. The IC50s are 0.01 µM, 0.01 µM, 0.06 µM, and 0.6 µM, respectively. In contrast, the KP-MRT-YM (YM) cell line is resistant to Palbociclib (IC50>10 µM). The flow cytometry results show that Palbociclib at concentrations between 0 to 1.0 µM induces G1 arrest in the AN, RY, G401 and NS cell lines in a concentration-dependent manner, but has no effect on YM cells. The BrdU incorporation results are consistent with the WST-8 and flow cytometry results: PD reduces BrdU incorporation (indicating G1 arrest) in the AN, RY, G401 and NS cell lines, but not in the YM cell line. Palbociclib, even at a concentration of 0.05 µM, significantly reduces BrdU incorporation in the AN, RY, and G401 cell lines (p<0.05).
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纯度及产品资料	98%

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