AS-0141
(Synonyms: Cdc7-IN-6) 目录号 : GC63375
AS-0141 (Cdc7-IN-6) 是一种有效的 Cdc7 激酶抑制剂 (IC50=4 nM)，具有抗肿瘤活性，详情请参考文献 WO2019165473A1，compound I-D。Cdc7 是一种丝氨酸苏氨酸蛋白激酶酶，在细胞周期中对 DNA 复制的启动至关重要。
Cas No.:1402057-88-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AS-0141 (Cdc7-IN-6) is a potent Cdc7 kinase inhibitor (IC50=4 nM), extracted from patent WO2019165473A1, compound I- D, has anti-tumor activity[1][2].
AS-0141 (Cdc7-IN-6) demonstrates potent inhibitory activity (IC50<3 µμ) in a range of solid tumor cell lines, including those of bladder (5673, RT1 12/84), sarcoma (143B, CADO-ES1, RD-ES, A673), colon and cecum (Colo-205, DLD-l, LS1034, SK-CO-l, SNU-C1), renal (U0.31), head-and-neck (CNE-2Z, RPMI-2650), melanoma (A2058, A875), and gastric (HGC-27) lineages[1].
[1]. Christian Andrew HASSIG, et al. Methods of treatment of cancer comprising cdc7 inhibitors. WO2019165473A1.
| Cas No. | 1402057-88-8 | SDF | |
| 别名 | Cdc7-IN-6 | ||
| 分子式 | C21H22F3N5O4 | 分子量 | 465.43 |
| 溶解度 | DMSO : 83.33 mg/mL (179.04 mM; Need ultrasonic) | 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 | 2.1486 mL | 10.7428 mL | 21.4855 mL |
| 5 mM | 0.4297 mL | 2.1486 mL | 4.2971 mL |
| 10 mM | 0.2149 mL | 1.0743 mL | 2.1486 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。
Discovery of AS-0141, a Potent and Selective Inhibitor of CDC7 Kinase for the Treatment of Solid Cancers
J Med Chem 2021 Oct 14;64(19):14153-14164.PMID:34607435DOI:10.1021/acs.jmedchem.1c01319
CDC7, a serine-threonine kinase, plays conserved and important roles in regulation of DNA replication and has been recognized as a potential anticancer target. We report here the optimization of a series of furanone analogues starting from compound 1 with a focus on ADME properties suitable for clinical development. By replacing the 2-chlorobenzene moiety in 1 with various aliphatic groups, we identified compound 24 as a potent CDC7 inhibitor with excellent kinase selectivity and favorable oral bioavailability in multiple species. Oral administration of 24 demonstrated robust in vivo antitumor efficacy in a colorectal cancer xenograft model. Compound 24 (AS-0141) is currently in phase I clinical trials for the treatment of solid cancers.