2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK12-IN-E9

CDK12-IN-E9 

Cat. No.: HY-117203A Purity: 99.97%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

CDK12-IN-E9 Chemical Structure

CDK12-IN-E9 Chemical Structure

CAS No. : 2020052-55-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 440 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 440 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 400 In-stock
Estimated Time of Arrival: December 31
10 mg USD 700 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2000 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target[1]

CDK12

 

CDK9/cyclinT1

23.9 nM (IC50)

cdk2/cyclin A

932 nM (IC50)

CDK7/Cyclin H/MNAT1

1210 nM (IC50)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Kelly, LAN5, SK-N-BE2, PC-9, NCI-H82 and NCI-H3122 cells
Concentration: 10 nM-10 μM
Incubation Time: 72 hours
Result: Showed potent antiproliferative activity in THZ1R NB and lung cancer cells, with IC50 values ranging from 8 to 40 nM.

Western Blot Analysis[1]

Cell Line: Kelly, PC-9, and NCI-H82 cells
Concentration: 0 nM, 30 nM, 100 nM, 300 nM, 1000 nM, 3000 nM
Incubation Time: 6 hours
Result: Led to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models.
Molecular Weight

434.53

Appearance

Solid

Formula

C24H30N6O2
CAS No.
SMILES

C=CC(NC1=CC=CC(NC2=CC(N3[[email protected]](CCO)CCCC3)=NC4=C(CC)C=NN24)=C1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (287.67 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 20.83 mg/mL (47.94 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.97%

COA (253 KB) HNMR (141 KB) RP-HPLC (246 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

CDK12-IN-E92020052-55-3CDKCyclin dependent kinaseCDK9CDK12antiproliferativeABCpyrazollopyridinephosphorylatedRNAPIIMYCMCL1Cys1039Inhibitorinhibitorinhibit

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