PD 0332991 (Palbociclib)
(Synonyms: 帕布昔利布（palbociclib）,PD0332991;PD-0332991;PD 0332991) 目录号 : GC15173
PD 0332991 (Palbociclib) (PD 0332991) 是一种具有口服活性的选择性 CDK4 和 CDK6 抑制剂，IC50 值分别为 11 和 16 nM。 PD 0332991 (Palbociclib) 具有有效的抗增殖活性，可诱导癌细胞的细胞周期停滞，可用于 HR 阳性和 HER2 阴性乳腺癌和肝细胞癌的研究。
Cas No.:571190-30-2
Sample solution is provided at 25 µL, 10mM.
PD-0332991 is selective and oral inhibitor of cyclin-dependent kinase 4/6 with IC50 values of 11nM and 16nM, respectively for CDK4 and CDK6 [1].
PD-0332991 is a highly specific inhibitor of CDK4/6. It is a potent anti-proliferative agent against Rb-positive tumor cells in vitro, subsequently inducing an exclusive G1 arrest. It has been reported to prevent tumor growth in disseminated human myeloma xenografts and induce G1 arrest in primary bone marrow cells [2].
PD-0332991 is also studied in breast cancer. It causes growth inhibition of ER-positive cell lines and 10/16 HER2-amplified cell lines. 100nM PD-0332991 can inhibit the phosphorylation of Rb in three more sensitive cell lines, resulting in prevention of cell cycle progression [2].
References:
[1] Ivan Diaz-Padilla, Lillian L. Siu and Ignacio Duran. Cyclin-dependent kinase inhibitors as potential targeted anticancer agents. Invest New Drugs. 2009, 27: 586–594.
[2] Richard S Finn, Judy Dering, Dylan Conklin, Ondrej Kalous, David J Cohen, Amrita J Desai, Charles Ginther, Mohammad Atefi, Isan Chen, Camilla Fowst, Gerret Los and Dennis J Slamon. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer ce
| Cell experiment: [1] | |
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Cell lines |
MDA-MB-453 cells |
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Preparation method |
The solubility of this compound in DMSO is |
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Reaction Conditions |
80 nM, 24 hours |
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Applications |
MDA-MB-453 breast carcinoma cells exposed to varying concentrations of PD 0332991 for 24 hours showed a significant increase in the percentage of cells in G1 in the presence of as little as 0.04 μmol/L PD 0332991 with a concomitant decline in other phases of the cell cycle. Maximum effects were attained at 0.08 μmol/L and an exclusive G1 arrest was maintained even at concentrations as high as 10 μmol/L, consistent with the complete absence of any other effects on the cell cycle. |
| Animal experiment: [1] | |
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Animal models |
Mice bearing Colo-205 colon carcinoma xenografts |
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Dosage form |
Oral administration, 150 or 75 mg/kg, daily for 14 days |
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Applications |
Administration of PD 0332991 produced rapid tumor regressions and a corresponding tumor growth delay of about 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 was obtained indicating a 90% inhibition of tumor growth rate. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Fry D W, Harvey P J, Keller P R, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Molecular cancer therapeutics, 2004, 3(11): 1427-1438. |
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| Cas No. | 571190-30-2 | SDF | |
| 别名 | 帕布昔利布（palbociclib）,PD0332991;PD-0332991;PD 0332991 | ||
| 化学名 | 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one | ||
| Canonical SMILES | CC(C(C(N1C2CCCC2)=N3)=CN=C3NC4=NC=C(N5CCNCC5)C=C4)=C(C1=O)C(C)=O | ||
| 分子式 | C24H29N7O2 | 分子量 | 447.53 |
| 溶解度 | 4.5mg/mL in DMSO（ultrasonic and warming and heat to 60°C) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2345 mL | 11.1724 mL | 22.3449 mL |
| 5 mM | 0.4469 mL | 2.2345 mL | 4.469 mL |
| 10 mM | 0.2234 mL | 1.1172 mL | 2.2345 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet