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Art. -Nr.: HY-181645

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CDK12-IN-9

CDK12-IN-9 is a potent and selective CDK12 inhibitor with an IC₅₀ of 2.2 nM. CDK12-IN-9 inhibits pSER2 (a downstream marker of CDK12/13 activity). CDK12-IN-9 can be used for the research of cancer.

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CAS. Nr.: 3024723-74-5
Formel: C₂₃H₂₀F₂N₁₀
Molecular Weight:474.47

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

CDK12-IN-9 Chemical Structure

CAS. Nr.: 3024723-74-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
Chemical Information
Protokoll (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CDK12

2.2 nM (IC₅₀)

CDK13

13 nM (IC₅₀)

CDK9

466 nM (IC₅₀)

CDK2

551 nM (IC₅₀)

CDK7

1491 nM (IC₅₀)

Alle CDK Isoform-spezifische Produkte anzeigen :

In Vitro

CDK12-IN-9 (Compound 17) potently inhibits purified CDK12 kinase with an IC₅₀ of 2.2 ± 0.74 nM^[1].
CDK12-IN-9 inhibits purified CDK13, CD9, CD7 and CD2 kinase with IC₅₀ values of 13, 466, 1491 and 551 nM^[1].
CDK12-IN-9 inhibits cellular pSER2 (a downstream marker of CDK12/13 activity) with an IC₅₀ of 17 ± 4.1 nM^[1].
CDK12-IN-9 inhibits pSER2 activity in whole blood with an IC₅₀ of 209 ± 106 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Parmacokinetics

Species	Dose	Route	C_max	AUC	T_1/2	F
Mice^[1]	0.2 mg/kg	i.v.	/	/	3.6 h	/
Mice^[1]	3 mg/kg	p.o.	1320 nM	9518 nM·h	/	72 %
Cynomolgus Monkey^[1]	0.3 mg/kg	p.o.	94 nM	983 nM·h	/	/
Dog^[1]	0.3 mg/kg	p.o.	137 nM	1035 nM·h	/	/

Chemical Information

CAS. Nr. 3024723-74-5
Molecular Weight 474.47
Formel C₂₃H₂₀F₂N₁₀
SMILES

N#CC1=CC2=C(N(C=N2)[C@H]3CCC[C@H](C3)NC4=NC=C(C(C5=CN(N=C5)CC(F)F)=N4)C#N)N=C1
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Protokoll

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Swyka R A, et al. Discovery of a Selective and Potent Inhibitor of Cyclin-Dependent Kinase 12/13 Employing a Noncovalent Mechanism[J]. ACS Medicinal Chemistry Letters, 2026.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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