PF-07104091
(Synonyms: (1R,3S)-3-(5-(3-(甲氧基甲基)-1-甲基-1H-吡唑-5-甲酰胺基)-1H-吡唑-3-基)环戊基异丙基氨基甲酸酯) 目录号 : GC62660
PF-07104091 is a CDK2/cyclin E1 inhibitor, a selective ATP-site inhibitor targeting the cyclin-bound activated state of the kinase [1].
Cas No.:2460249-19-6
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
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Preparation Method |
1000 cell/well were seeded in 384-well plate in 20 µL of RPMI 1640, or DMEM, respectively in 10% FBS at 37 °C, 5%CO2. Assay-ready plates containing 1:3 serial dilutions of compounds in 100% DMSO were prepared using acoustic dispensing technology (ECHO), final starting concentration was 20 µM. Compound-treated plates were incubated for 4 days (2 doubling times) and cell proliferation estimated using PI staining. |
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Reaction Conditions |
0-20µM for 4 days |
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Applications |
PF-07104091 inhibited T47D and KPL1 cells with IC50s of 0.785 and 0.603 µM, respectively. |
| Animal experiment [2]: | |
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Animal models |
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Preparation Method |
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References: [1]: Gharbi S I, Pelletier L A, Espada A, et al. Crystal structure of active CDK4-cyclin D and mechanistic basis for abemaciclib efficacy[J]. npj Breast Cancer, 2022, 8(1): 126. | |
PF-07104091 is a CDK2/cyclin E1 inhibitor, a selective ATP-site inhibitor targeting the cyclin-bound activated state of the kinase [1]. PF-07104091(Example 13) inhibited CDK2/cyclin E1, GSK3β, CDK1/cyclin A2, CDK4/cyclin D1, CDK6/cyclin D3 and CDK9, with Kis of 1.16, 537.81, 110, 238, 465 and 117 nM, respectively. PF-07104091 has anti-tumor activity for cyclin E1-amplified cancers. [1].
PF-07104091 inhibited T47D and KPL1 cells with IC50s of 0.785 and 0.603 µM, respectively [2].
The combination of abemaciclib and PF-07104091decreased T47D and KPL1 cells survival compared to either single agent [2].
References:
[1]. Behenna, D. C.; Freeman-Cook, K. D.; Hoffman, R. L.; Nagata, A.; Ninkovic, S.; Sutton, S. C. Preparation of aminopyrazolylcyclopentyl carbamate derivatives for use as CDK2 inhibitors. WO 2020157652, 2020.
[2]. Gharbi S I, Pelletier L A, Espada A, et al. Crystal structure of active CDK4-cyclin D and mechanistic basis for abemaciclib efficacy[J]. npj Breast Cancer, 2022, 8(1): 126.
PF-07104091 是一种 CDK2/cyclin E1 抑制剂，一种靶向激酶 [1] 的细胞周期蛋白结合激活状态的选择性 ATP 位点抑制剂。 PF-07104091（实施例 13）抑制 CDK2/细胞周期蛋白 E1、GSK3β；CDK1/细胞周期蛋白 A2、CDK4/细胞周期蛋白 D1、CDK6/细胞周期蛋白 D3 和 CDK9，Kis 分别为 1.16、537.81、110、238、465 和 117 nM . PF-07104091 对细胞周期蛋白 E1 扩增的癌症具有抗肿瘤活性。 [1].
PF-07104091 抑制 T47D 和 KPL1 细胞，IC50 分别为 0.785 和 0.603 µM，[2]。
与任一单一药物相比，abemaciclib 和 PF-07104091 的组合降低了 T47D 和 KPL1 细胞的存活率[2]。
| Cas No. | 2460249-19-6 | SDF | |
| 别名 | (1R,3S)-3-(5-(3-(甲氧基甲基)-1-甲基-1H-吡唑-5-甲酰胺基)-1H-吡唑-3-基)环戊基异丙基氨基甲酸酯 | ||
| 分子式 | C19H28N6O4 | 分子量 | 404.46 |
| 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 | 2.4724 mL | 12.3622 mL | 24.7243 mL |
| 5 mM | 0.4945 mL | 2.4724 mL | 4.9449 mL |
| 10 mM | 0.2472 mL | 1.2362 mL | 2.4724 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。