country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

製品番号: HY-151255

Copy Link Print Information

CDK8-IN-9

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC₅₀ value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2850253-95-9
分子式: C₂₄H₂₀F₃N₃O
分子量:423.43

保管条件:

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

Data Sheet (270 KB)

CDK8-IN-9 構造式

CAS 番号: 2850253-95-9

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC₅₀ value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies^[1].

CDK アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
CT26	GI₅₀	4 μM Compound: 22	Antiproliferative activity against mouse CT26 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against mouse CT26 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]
GES1	GI₅₀	61.5 μM Compound: 22	Cytotoxicity against human GES1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Cytotoxicity against human GES1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]
HCT-116	GI₅₀	4.9 μM Compound: 22	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]
HT-29	GI₅₀	4.3 μM Compound: 22	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]
SW480	GI₅₀	2.1 μM Compound: 22	Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay	[PMID: 36068975]

体外実験

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].

MedChemExpress (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 GI₅₀ 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.

体内実験

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].

MedChemExpress (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	-

Related Protocols :

化学情報

CAS 番号 2850253-95-9
分子量 423.43
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (270 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

お問い合わせ在庫あり

Other size

お問い合わせ