CDK5 inhibitor 20-223
目录号 : GC60680
CDK5inhibitor20-223是一种有效的CDK2和CDK5抑制剂，IC50分别为6.0和8.8nM。CDK5inhibitor20-223有潜力用于结肠直肠癌(CRC)的研究。
Cas No.:865317-30-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent[1].
CDK5 inhibitor 20-223 (10 nM-10 μM; 72 hours) potently inhibits cell growth in a panel of colorectal cancer (CRC) cell lines[1].CDK5 inhibitor 20-223 (0.3125-20 μM; 6 hours) induces a dose-dependent decrease in pRB (S807/811) and pFAK (S732) levels in each of the three CRC cell lines[1]. Cell Viability Assay[1] Cell Line: CRC cell lines SW620, DLD1, HT29, HCT116, FET, CBS, and GEO cells
CDK5 inhibitor 20-223 (8mg/kg; subcutaneously; for 14 injections) shows anti-tumor activity in human CRC xenograft tumors in nude mice[1]. Animal Model: Athymic nude mice[1]
[1]. Caroline M Robb, et al. Characterization of CDK(5) Inhibitor, 20-223 (Aka CP668863) for Colorectal Cancer Therapy. Oncotarget. 2017 Dec 28;9(4):5216-5232.
| Cas No. | 865317-30-2 | SDF | |
| Canonical SMILES | O=C(NC1=NNC(C2CCC2)=C1)CC3=CC=C4C=CC=CC4=C3 | ||
| 分子式 | C19H19N3O | 分子量 | 305.37 |
| 溶解度 | 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 | 3.2747 mL | 16.3736 mL | 32.7472 mL |
| 5 mM | 0.6549 mL | 3.2747 mL | 6.5494 mL |
| 10 mM | 0.3275 mL | 1.6374 mL | 3.2747 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。
A rapid and sensitive bioanalytical LC-MS/MS method for the quantitation of a novel CDK5 inhibitor 20-223 (CP668863) in plasma: Application to in vitro metabolism and plasma protein-binding studies
Biomed Chromatogr 2020 Aug;34(8):e4859.PMID:32307720DOI:10.1002/bmc.4859.
A rapid, selective, and sensitive liquid chromatography coupled with tandem mass spectrometry (MS/MS) method was developed and validated for the quantitation of the novel CDK5 inhibitor '20-223' in mouse plasma. Separation of analytes was achieved by a reverse-phase ACE Excel C18 column (1.7 μm, 100 × 2.1 mm) with gradient elution using 0.1% formic acid (FA) in methanol and 0.1% FA as the mobile phase. Analytes were monitored by MS/MS with an electrospray ionization source in the positive multiple reaction monitoring mode. The MS/MS response was linear over the concentration range 0.2-500 ng/mL for 20-223. The within- and between-batch precision were within the acceptable limits as per Food and Drug Administration guidelines. The validated method was successfully applied to plasma protein binding and in vitro metabolism studies. Compound 20-223 was highly bound to mouse plasma proteins (>98% bound). Utilizing mouse S9 fractions, in vitro intrinsic clearance (CLint ) was 24.68 ± 0.99 μL/min/mg protein. A total of 12 phase I and II metabolites were identified with hydroxylation found to be the major metabolic pathway. The validate method required a low sample volume, was linear from 0.2 to 500 ng/mL, and had acceptable accuracy and precision.