Palbociclib monohydrochloride - CAS:827022-32-2

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Palbociclib monohydrochloride (Synonyms:PD 0332991 monohydrochloride)

目录号 : KM16327 CAS No. : 827022-32-2 纯度 : 98%

Data Sheet 产品使用指南

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。

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100mg		In-stock
200mg		In-stock
500mg		In-stock
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5g	询价	In-stock

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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.

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).

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.

分子式

C₂₄H₂₉N₇O₂^.ClH

分子量

483.99

CAS号

827022-32-2

中文名称

帕布昔利布盐酸盐；帕博西林盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

H₂O : 50 mg/mL (103.31 mM; Need ultrasonic)

DMSO : 5 mg/mL (10.33 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0662 mL	10.3308 mL	20.6616 mL
5 mM	0.4132 mL	2.0662 mL	4.1323 mL
10 mM	0.2066 mL	1.0331 mL	2.0662 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： Lactic acid buffer (50 mM, pH 4.0)
Solubility: 4.17 mg/mL (8.62 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.54 mg/mL (1.12 mM); Clear solution

此方案可获得 ≥ 0.54 mg/mL (1.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.4 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.54 mg/mL (1.12 mM); Clear solution

此方案可获得 ≥ 0.54 mg/mL (1.12 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.4 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

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浓度

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Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 71 篇科研文献

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