2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. 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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CDK9-IN-40

CDK9-IN-40 Chemical Structure

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CDK9-IN-40 Related Antibodies

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Description

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[1].

IC50 & Target[1]

CDK9

5.5 nM (IC50)

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.

CDK9-IN-40 Related Antibodies

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[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. T1/2 6.5 hr
Rat 10 mg/kg p.o. T1/2 3.6 hr
Rat 1 mg/kg i.v. Tmax 0.083 hr
Rat 10 mg/kg p.o. Tmax 4.0 hr
Rat 1 mg/kg i.v. MRT0-t 5.4 hr
Rat 10 mg/kg p.o. MRT0-t 125.2 hr
Rat 1 mg/kg i.v. MRT0-∞ 8.4 hr
Rat 10 mg/kg p.o. MRT0-∞ 155.8 hr
Rat 1 mg/kg i.v. AUC0-t 26.5 ng·h/mL
Rat 10 mg/kg p.o. AUC0-t 6.9 ng·h/mL
Rat 1 mg/kg i.v. AUC0-∞ 33.1 ng·h/mL
Rat 10 mg/kg p.o. AUC0-∞ 7.9 ng·h/mL
Rat 1 mg/kg i.v. CL 51.9 L/h/kg
Rat 10 mg/kg p.o. CL 117.2 L/h/kg
Rat 1 mg/kg i.v. Vz 375.3 L/kg
Rat 10 mg/kg p.o. Vz 628.7 L/kg
Rat 1 mg/kg i.v. Cmax 15.9 ng/mL
Rat 10 mg/kg p.o. Cmax 18.6 ng/mL
Rat 10 mg/kg p.o. F 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.
Molecular Weight

422.55

Formula

C21H26N8S
SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC(N4CCC5=C(SC(N)=N5)C4)=CC=N3
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
References
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CDK9-IN-40 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK9-IN-40CDKApoptosisCyclin dependent kinaseAntiproliferative activityCDK9Structure-activity relationshipTetrahydrothiazolopyridineInhibitorinhibitorinhibit

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