CDK/CRK Inhibitor
(Synonyms: Cdk7 Inhibitor IV, Cyclin-dependent kinase 7 Inhibitor IV, Cyclin-dependent kinase/CDK-related kinase Inhibitor, RGB-286147) 目录号 : GC43217
A CDK/CRK-specific kinase inhibitor
Cas No.:784211-09-2
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
CDK/CRK inhibitor is an inhibitor of cyclin-dependent kinases (CDK) and CDK-related kinases (CRK) with IC50 values ranging from 9-839 nM in vitro. It is selective, exhibiting less than 20% inhibition of 60 non-CDK/CRK kinases, at a concentration of 1 μM. CDK/CRK inhibitor induces cell cycle arrest in the G1 phase, endoreduplication, and apoptosis in HCT116 cells. It exhibits broad anti-tumor activity with an average GI50 value of <10 nM for 60 tumorigenic cell lines. It also inhibits growth of non-cycling HCT116 cells with an IC50 value of 40 nM.
| Cas No. | 784211-09-2 | SDF | |
| 别名 | Cdk7 Inhibitor IV, Cyclin-dependent kinase 7 Inhibitor IV, Cyclin-dependent kinase/CDK-related kinase Inhibitor, RGB-286147 | ||
| Canonical SMILES | O=C1C2=C(N(C3=C(Cl)C=CC=C3Cl)N=C2C(C)C)NC(CC4=CC=C(OCCO)C=C4)=N1 | ||
| 分子式 | C23H22Cl2N4O3 | 分子量 | 473.4 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml | 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 | 2.1124 mL | 10.5619 mL | 21.1238 mL |
| 5 mM | 0.4225 mL | 2.1124 mL | 4.2248 mL |
| 10 mM | 0.2112 mL | 1.0562 mL | 2.1124 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。
Combination screening in vitro identifies synergistically acting KP372-1 and cytarabine against acute myeloid leukemia
Biochem Pharmacol 2016 Oct 15;118:40-49.PMID:27565890DOI:10.1016/j.bcp.2016.08.020
Cytogenetic lesions often alter kinase signaling in acute myeloid leukemia (AML) and the addition of kinase inhibitors to the treatment arsenal is of interest. We have screened a kinase inhibitor library and performed combination testing to find promising drug-combinations for synergistic killing of AML cells. Cytotoxicity of 160 compounds in the library InhibitorSelect™ 384-Well Protein Kinase Inhibitor I was measured using the fluorometric microculture cytotoxicity assay (FMCA) in three AML cell lines. The 15 most potent substances were evaluated for dose-response. The 6 most cytotoxic compounds underwent combination synergy analysis based on the FMCA readouts after either simultaneous or sequential drug addition in AML cell lines. The 4 combinations showing the highest level of synergy were evaluated in 5 primary AML samples. Synergistic calculations were performed using the combination interaction analysis package COMBIA, written in R, using the Bliss independence model. Based on obtained results, an iterative combination search was performed using the therapeutic algorithmic combinatorial screen (TACS) algorithm. Of 160 substances, cell survival was ⩽50% at <0.5μM for CDK/CRK Inhibitor, KP372-1, synthetic fascaplysin, herbimycin A, PDGF receptor tyrosine kinase inhibitor IV and reference-drug cytarabine. KP372-1, synthetic fascaplysin or herbimycin A obtained synergy when combined with cytarabine in AML cell lines MV4-11 and HL-60. KP372-1 added 24h before cytarabine gave similar results in patient cells. The iterative search gave further improved synergy between cytarabine and KP372-1. In conclusion, our in vitro studies suggest that combining KP372-1 and cytarabine is a potent and synergistic drug combination in AML.