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CDK12-IN-4

Name: CDK12-IN-4
Brand: TargetMol
SKU: T40288
Rating: 4.5 (1 reviews)

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Catalog No. T40288Cas No. 2651196-69-7

Alias CDK12-IN-4

CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).

CDK12-IN-4

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Catalog No. T40288Alias CDK12-IN-4Cas No. 2651196-69-7

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5 mg	$970	Backorder

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Product Introduction

Bioactivity

Description	CDK12-IN-4, a pyrazolotriazine compound, exhibits potent inhibition of CDK12 by achieving an IC50 value of 0.641 μM, utilizing high ATP levels (2 mM). Notably, CDK12-IN-4 does not impact CDK2/Cyclin E (IC50 > 20 μM) or CDK9/Cyclin T1 (IC50 > 20 μM) under the influence of high ATP (2 mM) levels (WO2021116178A1).
Targets&IC50	CDK9-CyclinT1:>20 μM (IC50), CDK2-CyclinE:>20 μM (IC50), CDK12:0.641 μM (IC50)
In vitro	CDK12-IN-4 (Example 172) selectively inhibits BRCA1 mRNA expression in MDA-MB-231 cells with an IC50 value of 0.626 nM, without affecting CAL-120 cells. It demonstrates antiproliferative effects in MDA-MB-231 and CAL-120 cells, with IC50 values of 0.535 nM and 2.43 nM, respectively, and a high CDK12 inhibition potency with an IC50 to degradation DC50 ratio of 581, indicating effectiveness and selective action [1].
Alias	CDK12-IN-4

Chemical Properties

Molecular Weight	426.432
Formula	C₂₀H₂₀F₂N₈O
Cas No.	2651196-69-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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Keywords

CDK-12-IN-4CDK12IN4CDK12 IN 4