[CAS NO. 2220184-50-7]  CDK12-IN-3

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PRODUCTS SPECIFICATIONS [2220184-50-7]

Distributor
Catalog
AS928176
Brand
Arctom Scientific
CAS
2220184-50-7

DESCRIPTION [2220184-50-7]

Overview

MDL-
Molecular Weight470.52
Molecular FormulaC23H28F2N8O
SMILESCC(C)N1C2=NC(N3CCCC[C@H]3CCO)=NC(NCC4=NC5=C(C(F)=C(F)C=C5)N4)=C2N=C1

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

Summary

CDK12-IN-3 is a potent and selective CDK12 inhibitor with an IC 50 of 491 nM in enzymatic assay.


IC50 & Target

CDK12

491 nM (IC 50 )


In Vitro

CDK12-IN-3 is a highly selective CDK12 inhibitor profiled across a panel of 352 kinases at 0.1 µM. CDK12-IN-3 shows potent inhibition of phosphorylation of Ser2 on the CTD repeat domain of RNA Pol II as well as growth inhibition of OV90 cells and acute cytotoxicity to THP1 cells [1] .

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


Appearance

Solid


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 : 250 mg/mL ( 531.33 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1253 mL 10.6265 mL 21.2531 mL
5 mM 0.4251 mL 2.1253 mL 4.2506 mL
10 mM 0.2125 mL 1.0627 mL 2.1253 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.33 mg/mL (4.95 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.33 mg/mL (4.95 mM); Clear solution

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