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CDK12-IN-6

Name: CDK12-IN-6
Brand: TargetMol
SKU: T40289
Rating: 4.5 (1 reviews)

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Catalog No. T40289Cas No. 2651196-71-1

Alias CDK12-IN-6

CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).

CDK12-IN-6

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Catalog No. T40289Alias CDK12-IN-6Cas No. 2651196-71-1

Pack Size	Price	Availability	Quantity
5 mg	$970	Backorder

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Product Introduction

Bioactivity

Description	CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).
Targets&IC50	CDK12:1.19 μM (IC50), CDK2-CyclinE:>20 μM (IC50), CDK9-CyclinT1:>20 μM (IC50)
In vitro	CDK12-IN-6 (Example 174) suppresses BRCA1 mRNA expression in MDA-MB-231 cells with an IC50 of 0.872 nM, while having no impact on CAL-120 cells. It also demonstrates antiproliferative effects in both MDA-MB-231 (IC50 = 2.19 nM) and CAL-120 cells (IC50 = 1 nM). Moreover, CDK12-IN-6 exhibits high CDK12 inhibition efficiency with an IC50 to DC50 ratio of 1851, indicating potent activity in hindering CDK12 in ATP to degradation processes.
Alias	CDK12-IN-6

Chemical Properties

Molecular Weight	425.448
Formula	C₂₀H₂₁F₂N₉
Cas No.	2651196-71-1
Relative Density.	no data available

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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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

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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-6CDK12IN6CDK12 IN 6