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Cat. No.: HY-176736

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CDK9-IN-40

CDK9-IN-40 is a potent and orally active CDK9 inhibitor with an IC₅₀ of 5.5 nM. CDK9-IN-40 shows high selectivity for CDK9 versus CDK1, CDK2, CDK4, and CDK6, respectively. CDK9-IN-40 can arrest cell cycle, induce cell apoptosis and inhibit tumor growth. CDK9-IN-40 exhibits strong anti-cancer activity.

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화학식: C₂₁H₂₆N₈S
분자량:422.55

보관:

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

Data Sheet (270 KB)

CDK9-IN-40 Chemical Structure

사이즈

가격

재고

수량

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

CDK9

5.5 nM (IC₅₀)

All CDK Isoforms :

In Vitro

CDK9-IN-40 (Compound 8e) (1.0 μM, 48 h) exhibits the highest inhibitory activities against CDK9 (99% inhibition, IC₅₀ = 5.5 nM) and shows over 180 and 75-fold selectivity for CDK9 versus CDK1 and CDK2, respectively^[1].
CDK9-IN-40 (1.8 μM-3.0 μM, 48 h) possesses remarkable cell growth inhibitory activity toward HeLa, A549, HCT116, and MCF-7 cells, which are greater or similar with ZK304709^[1].
CDK9-IN-40 (1 μM-4 μM, 24 h) can cause the G2/M phase arrest and induce cell apoptosis in HCT116 cells in a concentration-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:

HeLa, A549, HCT116, MCF-7, HEK293, LO2
Concentration:

1 μM
Incubation Time:

48 h
Result:

Offered the best CDK9 inhibitory activities (IC₅₀ = 5.5 nM), being comparable to that of ZK304709 (IC₅₀ = 5.0 nM) and higher than AZD5438 (IC₅₀ = 18.0 nM).
Didn’t demonstrate obvious cytotoxic activity against two non-tumoural cells HEK-293 and LO2 (IC₅₀ = 50 μM).

Cell Cycle Analysis^[1]

Cell Line:

HCT116
Concentration:

1.0 μM, 2.0 μM, 4.0 μM
Incubation Time:

24 h
Result:

Induced a dose-dependent G2/M phase arrest (14.71%, 18.16%, and 24.81% respectively).

Apoptosis Analysis^[1]

Cell Line:

HCT116
Concentration:

1.0 μM, 2.0 μM, 4.0 μM
Incubation Time:

24 h
Result:

Induced total apoptosis rates of 10.08%, 16.43%, and 33.70% with the rate of 1.0, 2.0 and 4.0 μM, respectively.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	MRT_0-t	MRT_0-∞	AUC_0-t	AUC_0-∞	CL	V_z	C_max	F
Rat^[1]	1 mg/kg	i.v.	6.5 h	0.083 h	5.4 h	8.4 h	26.5 ng·h/mL	33.1 ng·h/mL	51.9 L/h/kg	375.3 L/kg	15.9 ng/mL	/
Rat^[1]	10 mg/kg	p.o.	3.6 h	4.0 h	125.2 h	155.8 h	6.9 ng·h/mL	7.9 ng·h/mL	117.2 L/h/kg	628.7 L/kg	18.6 ng/mL	41.7 %

In Vivo

CDK9-IN-40 (Compound 8e) (60 mg/kg, PO, once daily, for 7 days) exhibits potent in vivo antitumor activity in HCT116 xenograft mouse models with tumor growth inhibition of 59.2%^[1].

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

Animal Model:

Four-week-old pathogen-free male Balb/c-nu mice were used to establish HCT116 xenograft models ^[1]
Dosage:

30 mg/kg, 60 mg/kg
Administration:

Oral gavage (PO); Once daily; for 7 days; 4 days after cell injection
Result:

Exhibited potent antitumor effects, suppressing tumor growth by 59.2% at a dose of 60 mg/kg per day.

Chemical Information

분자량 422.55
화학식 C₂₁H₂₆N₈S
SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC(N4CCC5=C(SC(N)=N5)C4)=CC=N3
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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]. Chen L et al. Discovery and optimization of novel tetrahydrothiazolopyridine-based pyrimidines as highly potent cyclin-dependent kinase 9 (CDK9) inhibitors. Eur J Med Chem. 2025 Jun 14;296:117875. doi: 10.1016. https://pubmed.ncbi.nlm.nih.gov/40544651/

[2]. Chen L et al. Discovery and optimization of novel tetrahydrothiazolopyridine-based pyrimidines as highly potent cyclin-dependent kinase 9 (CDK9) inhibitors. Eur J Med Chem. 2025 Jun 14;296:117875. doi: 10.1016. [Content Brief]

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

CDK9-IN-40

All CDK Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

CDK9-IN-40 Related Classifications

HY-176736 Related Classifications