[CAS NO. 2850253-95-9] CDK8-IN-9

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PRODUCTS SPECIFICATIONS [2850253-95-9]

Catalog

HY-151255

Brand

MCE

CAS

2850253-95-9

DESCRIPTION [2850253-95-9]

Overview

MDL	-
Molecular Weight	423.43
Molecular Formula	C24H20F3N3O
SMILES	O=C(NC1=CC=C(C)C(C(F)(F)F)=C1)CCC2=CC=CC(C3=CN=C(NC=C4)C4=C3)=C2

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

Summary

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC ₅₀ value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies ^[1] .

In Vitro

CDK8-IN-9 (compound 22) (0-100 μM, 48 h) can significantly inhibit cell proliferation and target CDK8 to inhibit the activation of the WNT/β-catenin pathway, thereby suppressing β-catenin-mediated transcriptional activity of TCF/ LEF ^[1] .
CDK8-IN-9 (compound 22) (0.5,1 and 2 μM, 24 h) induces G2/M and S-phase cell cycle arrest, thereby inhibiting cell proliferation rather than inducing apoptosis ^[1] .

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

Cell Viability Assay ^[1]

Cell Line:	HCT-116, HT-29, SW-480, CT-26 and GES-1 cells
Concentration:	0-100 μM
Incubation Time:	48 hours
Result:	Inhibited HCT-116, HT-29, SW-480, CT-26 and GES-1 cells with the GI ₅₀ values of 4.9, 4.3, 2.1, 4.0 and 61.5 μM, respectively.

Cell Cycle Analysis ^[1]

Cell Line:	HCT-116 cells
Concentration:	0.5, 1, and 2 μM
Incubation Time:	24 hours
Result:	Arrested cells in G2/M phase by 17%, 20.26% and 34.45% at concentrations of 0.5, 1, and 2 μM, respectively. Showed a decrease in the G0/G1 phase and a slight increase in the S phase.

In Vivo

CDK8-IN-9 (compound 22) (p.o., 20, 40 and 80 mg/kg, daily, 3 weeks) significantly reduces in tumor volume and inhibits weight loss in mice at the concentration of 80 mg/kg in Balb/c mice infected with CT-26 murine colon cancer cells ^[1] .

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

Animal Model:

Sprague−Dawley rats ^[1]

Dosage:

10 mg/kg or 5 mg/kg

Administration:

p.o. for 10 mg/kg and i.v. for 5 mg/kg

Result:

The pharmacokinetic parameters of CDK8-IN-9 (compound 22)

Parameters	t _1/2 (h)	T _max (h)	MRT (h)	C _max (μg/L)	AUC _0-∞ (μg/L·h)	CL (L/h/kg)	F (%)
10 mg/kg (po)	1.21	0.75	2.022	497.56	783.66	9.23	39.8
5 mg/kg (iv)	1.63	-	1.756	706.29	983.09	11.32	-

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Storage

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

References

[1] Xing Xing Zhang, et al. Discovery of the Novel 1H-Pyrrolo[2,3-b]pyridine Derivative as a Potent Type II CDK8 Inhibitor against Colorectal Cancer. J. Med. Chem.