规格 | 价格 | |
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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
靶点 |
DYRK1A 2000 nM (IC50) MAPK 8000 nM (IC50) Cdk4/cyclin D3 9 nM (IC50) Cdk4/cyclin D1 11 nM (IC50) Cdk6/cyclin D2 16 nM (IC50)
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体外研究 (In Vitro) |
palbociclib (0-1 μM, 24 h) 乳清酸盐抑制 MDA-MB-435 细胞视网膜母细胞瘤中 Ser795 的磷酸化,IC50 值为 0.063 μM。它还对结肠癌 Colo-205 中 Ser780 和 Ser795 的磷酸化具有类似的影响[1]。仅处于 G1 期的 MDA-MB-453 细胞会被 palbociclib(0–10 μM,24 小时)乳清酸盐抑制[1]。在 MDA-MB-453 和 MDA-MB-361 细胞中,palbociclib(500 nM,7 天)乳清酸盐增强同源基因(H2d1、H2k1 和 B2m)的表达[2]。 palbociclib(0-1 μM,6 天)乳清酸盐可抑制多种管腔 ER 阳性和 HER2 扩增乳腺癌细胞系的生长,IC50 值范围为 0.01 μM 至 3.49 μM。此外,palbociclib(0-1 μM,3 天)乳清酸盐可抑制人肝癌细胞系的增殖,导致可逆的细胞周期停滞[4]。
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体内研究 (In Vivo) |
Palbociclib 以 75 或 150 mg/kg 的剂量口服 14 天时,会导致肿瘤发展更慢并迅速消退[1]。用 Palbociclib(口服,90 mg/kg,每天,持续 12 天)治疗的无肿瘤动物,脾脏和淋巴结中的 Treg 计数以及 Treg:CD8 比率降低,表明与肿瘤无关的作用[2]。 Palbociclib,乳清酸盐(口服治疗,100 mg/kg,每天一次,持续 1 周)在基因改变肝癌的嵌合小鼠模型中表现出强大的抗肿瘤作用[4]。
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细胞实验 |
细胞增殖检测[3]
细胞类型: ER 阳性以及 HER2 扩增的乳腺癌细胞系(MDA-MB-175、ZR-75-30、CAMA-1 等) .) 测试 测试浓度: 0-1 μM 孵育时间: 6 天 实验结果: 抑制生长Luminal ER 阳性以及 HER2 扩增的乳腺癌细胞系。 细胞周期分析sup>[1] 细胞类型: MDA-MB-453 细胞测试 测试浓度: 0-1 μM 孵育时间::24小时 实验结果:G1期停滞的MDA-MB-453细胞。 |
动物实验 |
Animal/Disease Models: Mice bearing Colo-205 colon carcinoma xenografts (p16 deleted)[1]
Doses: 75, 150 mg/kg Route of Administration: Oral administration; daily for 14 days Experimental Results: Produced rapid tumor regressions and a corresponding tumor growth delay of ~50 days. Animal/Disease Models: Tumor-free female FVB mice[2] Doses: 90 mg/kg Route of Administration: Oral administration; daily for 12 days Experimental Results: decreased total thymic mass and immature CD4+ and CD8+ double-positive thymocytes, and increased the fractions of CD4+ and CD8+ single-positive thymocytes. Animal/Disease Models: Genetically engineered mosaic mouse model of liver cancer (Myc;p53-sgRNA)[4] Doses: 100 mg/kg Route of Administration: Oral administration; daily for 1 week Experimental Results: diminished the luminescence signal in liver and delayed tumor growth. |
参考文献 |
[1]. Fry DW, et al. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38.
[2]. Goel S, et al. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017 Aug 24;548(7668):471-475. [3]. Richard S Finn, et al. PD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro. Breast Cancer Res. 2009;11(5):R77. [4]. Bollard J, et al. Palbociclib (PD-0332991), a selective CDK4/6 inhibitor, restricts tumour growth in preclinical models of hepatocellular carcinoma. Gut. 2017 Jul;66(7):1286-1296. |
分子式 |
C29H33N9O6
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分子量 |
603.63
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CAS号 |
2757498-64-7
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相关CAS号 |
Palbociclib;571190-30-2;Palbociclib monohydrochloride;827022-32-2;Palbociclib hydrochloride;571189-11-2;Palbociclib dihydrochloride
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溶解度 (体内) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
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制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6566 mL | 8.2832 mL | 16.5664 mL | |
5 mM | 0.3313 mL | 1.6566 mL | 3.3133 mL | |
10 mM | 0.1657 mL | 0.8283 mL | 1.6566 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。