CDK12-IN-E9 |
| Catalog No.GC60103 |
CDK12-IN-E9는 강력하고 선택적인 공유 CDK12 억제제이자 비공유 CDK9 억제제이며 ABC 수송체 매개 유출을 피합니다. CDK12-IN-E9는 IC50> 1 μM으로 CDK7/CyclinH 복합체에 약한 결합 능력을 가지고 있습니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2020052-55-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and a non-covalent CDK9 inhibitor, while avoiding ABC transporter-mediated efflux. CDK12-IN-E9 has weak binding ability to CDK7/CyclinH complex with an IC50> 1 μM[1].
CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM[1].CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression[1].CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9[1]. Cell Proliferation Assay[1] Cell Line: Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells
[1]. Gao Y, et al. Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors. Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5.
| Cas No. | 2020052-55-3 | SDF | |
| Canonical SMILES | C=CC(NC1=CC=CC(NC2=CC(N3[C@H](CCO)CCCC3)=NC4=C(CC)C=NN24)=C1)=O | ||
| Formula | C24H30N6O2 | M.Wt | 434.53 |
| Solubility | Storage | ||
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3013 mL | 11.5067 mL | 23.0134 mL |
| 5 mM | 0.4603 mL | 2.3013 mL | 4.6027 mL |
| 10 mM | 0.2301 mL | 1.1507 mL | 2.3013 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *