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CDK12-IN-E9

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Catalog No. T14915Cas No. 2020052-55-3

CDK12-IN-E9 is a cell cycle protein kinase (CDK) inhibitor with anticancer and antitumor activity that can be used in the study of breast cancer.

CDK12-IN-E9

CDK12-IN-E9

🥰Excellent
Catalog No. T14915Cas No. 2020052-55-3
CDK12-IN-E9 is a cell cycle protein kinase (CDK) inhibitor with anticancer and antitumor activity that can be used in the study of breast cancer.
Pack SizePriceAvailabilityQuantity
1 mg$193In Stock
5 mg$486In Stock
10 mg$728In Stock
25 mg$1,352In Stock
1 mL x 10 mM (in DMSO)$535In Stock
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Product Introduction

Bioactivity
Description
CDK12-IN-E9 is a cell cycle protein kinase (CDK) inhibitor with anticancer and antitumor activity that can be used in the study of breast cancer.
Targets&IC50
CDK2-CyclinA:932 nM, CDK7-CyclinH-MNAT1:1210 nM, CDK9-CyclinT1:23.9 nM
In vitro
CDK12-IN-E9 treatment of Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82, and NCI-H3122 cells after 72 hours of action in the concentration range of 10 nM to 10 μM showed significant antiproliferative activity against THZ1R neuroblastoma and lung cancer cells, with IC50 values ranging from 8 to 40 nM.
After 6 hours of action in the concentration range of 0 to 3000 nM, CDK12-IN-E9 treatment of Kelly, PC-9, and NCI-H82 cells induced a dose-dependent decrease in phosphorylated and total RNAPII accompanied by a decrease in MYC and MCL1 expression in THZ1R neuroblastoma and lung cancer models.
In addition, CDK12-IN-E9 increased PARP cleavage and elevated the proportion of sub-G1 phase cells in THZ1R lung cancer cells, whereas it was more likely to cause G2/M phase block in neuroblastoma cells after 24 hours of exposure. [1]
Chemical Properties
Molecular Weight434.53
FormulaC24H30N6O2
Cas No.2020052-55-3
SmilesC(C)C1=C2N(C(NC3=CC(NC(C=C)=O)=CC=C3)=CC(=N2)N4[C@H](CCO)CCCC4)N=C1
Relative Density.1.28 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 100 mg/mL (230.13 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3013 mL11.5067 mL23.0134 mL115.0669 mL
5 mM0.4603 mL2.3013 mL4.6027 mL23.0134 mL
10 mM0.2301 mL1.1507 mL2.3013 mL11.5067 mL
20 mM0.1151 mL0.5753 mL1.1507 mL5.7533 mL
50 mM0.0460 mL0.2301 mL0.4603 mL2.3013 mL
100 mM0.0230 mL0.1151 mL0.2301 mL1.1507 mL

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