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Cat. No.: HY-162619

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CDK9-IN-33

CDK9-IN-33 (compound C35) is a potent, selective and orally active CDK9 inhibitor with IC₅₀ values of 17.44, 160, 316.30, 1771.00, >10000 nM for CDK9, CDK7, CDK2, CDK4, CDK6 respectively. CDK9-IN-33 induces apoptosis. CDK9-IN-33 decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1. CDK9-IN-33 shows anti-tumor activity.

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

Formula: C₂₃H₃₁N₇O₂
Molecular Weight:437.54

Storage:

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

Data Sheet (275 KB)

CDK9-IN-33 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

CDK9

17.44 nM (IC₅₀)

CDK7

160 nM (IC₅₀)

CDK2

316.30 nM (IC₅₀)

CDK4

1771.00 nM (IC₅₀)

CDK6

>10000 nM (IC₅₀)

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	20.08 nM Compound: C35	Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay Inhibition of cell viability in mouse 4T1 cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
BT-549	IC₅₀	5.61 nM Compound: C35	Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay Inhibition of cell viability in human BT-549 cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
MDA-MB-231	IC₅₀	5.9 nM Compound: C35	Inhibition of cell viability in human MDA-MB-231 cells incubated for 4 days by WST-8 assay Inhibition of cell viability in human MDA-MB-231 cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
MDA-MB-468	IC₅₀	10.05 nM Compound: C35	Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay Inhibition of cell viability in human MDA-MB-468 cells incubated for 4 days by WST-8 assay	[PMID: 38885173]
MM1.S	IC₅₀	2438 nM Compound: C35	Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay Inhibition of cell viability in human MM1.S cells incubated for 4 days by WST-8 assay	[PMID: 38885173]

In Vitro

CDK9-IN-33 (compound C35) (0, 0.01, 0.1, 1 µM; 24 h) decreases the protein expression of RPB1 CTD Ser2, RPB1, MCL1 and increases the expression of cleaved PARP^[1].
CDK9-IN-33 (0, 0.01, 0.1, 1 µM) decreases the mRNA expression levels of the MCL1 gene^[1].
. CDK9-IN-33 (0, 0.01, 0.1, 1 µM; 72 h) induces apoptosis in a dose-dependent manner^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-231, MDA-MB-468, BT549, 4T1, mino, MM.1S cells
Concentration:
Incubation Time:

4 days
Result:

Showed antiproliferation potential for MDA-MB-231, MDA-MB-468, BT549, 4T1, mino, MM.1S cells with IC₅₀ values of 5.9, 10.05, 5.61, 20.08, 8.98, 24.38 nM, respectively.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

0, 0.01, 0.1, 1 µM
Incubation Time:

24 h
Result:

Showed a dose-dependent inhibition on the phosphorylation of RPB1 CTD Ser2, RPB1, increased the protein of cleaved PARP.

RT-PCR^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

0, 0.01, 0.1, 1 µM
Incubation Time:

24 h
Result:

Showed a dose-dependent inhibition on the phosphorylation of RPB1 CTD Ser2, RPB1, increased the protein of cleaved PARP.

Apoptosis Analysis^[1]

Cell Line:

4T1 cells
Concentration:

0, 0.01, 0.1, 1 µM
Incubation Time:

72 h
Result:

Induced apoptosis in a dose-dependent manner.

In Vivo

CDK9-IN-33 (10 mg/kg; p.o.; daily for 10 days) shows anti-tumor activity in mice^[1].
Pharmacokinetic Parameters (male ICR mice; p.o. 20.0 mg/kg, i.v. 5.0 mg/kg; )^[1].

Cmpd	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_0-t (h·ng/mL)	AUC_t–∞ (h·ng/mL)	CL (mL/min/kg)	MRT_0–∞ (h)	V_ss (mL/kg)	F (%)
C35 (p.o.)	0.68	0.5	2867	4349	4350	-	1.43	-	68.9
C35 (i.v.)	0.36	-	-	1578	1578	52.9	0.33	1033	-

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

Chemical Information

Molecular Weight 437.54
Formula C₂₃H₃₁N₇O₂
SMILES

CC(C1=C2N=C(N=C(N2N=C1)NCC3=CC=C(C=C3)NC(CC)=O)NC4CCOCC4)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 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)

References

[1]. Wang WJ, et al. Discovery of Orally Bioavailable and Potent CDK9 Inhibitors for Targeting Transcription Regulation in Triple-Negative Breast Cancer. J Med Chem. 2024 Jun 27;67(12):10035-10056. [Content Brief]

Calculators

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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.

Keywords

100 mg

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