CHK1-IN-4 hydrochloride

製品番号: HY-128766A: Data Sheet 取扱説明書
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CHK1-IN-4 hydrochloride is a selective checkpoint kinase 1 (Chk1) inhibitor with an IC₅₀ ≤ 1 nM. The IC₅₀ value of CHK1-IN-4 hydrochloride against Chk2 ranges from 50 to 100 nM. CHK1-IN-4 hydrochloride inhibits cancer cell proliferation and exhibits antitumor activity in colon cancer xenograft models. CHK1-IN-4 hydrochloride can be used for the research of colon cancer and breast cancer.

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。

CHK1-IN-4 hydrochloride 構造式

容量	価格（税別）	在庫状況	数量
1 mg	$330	在庫あり	Estimated Time of Arrival: December 31
5 mg	$820	在庫あり	Estimated Time of Arrival: December 31
10 mg		お問い合わせ
50 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

Other Forms of CHK1-IN-4 hydrochloride:

CHK1-IN-4 お問い合わせ

Checkpoint Kinase (Chk) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

Chk1 Chk2 BUBR1

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

IC₅₀ & Target^[1]

Chk1

≤ 1 nM (IC₅₀)

体外実験

CHK1-IN-4 (Compound 3) hydrochloride inhibits the proliferation of HT-29 colon cancer cells and MDA-MB-231 breast cancer cells, with IC₅₀ values ranging from 10-50 nM and 50-100 nM, respectively^[1].
CHK1-IN-4 (0.4-33.3 nM; 16.5-27 h) hydrochloride potently inhibits SN-38 (HY-13704)-induced Chk1^S296 phosphorylation in HT-29 colon cancer cells^[1].

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

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-t	AUC_0-inf	MRT	V_d	V_ss	Clearance (CL)
Rat^[1]	10 mg/kg	i.v.	3.8 h	4531 ng/mL·h	4637 ng/mL·h	2.8 h	12.3 L/kg	6.4 L/kg	2.3 L/h/kg

体内実験

CHK1-IN-4 (Compound 3) (40 mg/kg; intravenous injection; twice weekly) hydrochloride exhibits potent tumor growth inhibitory activity in the HT-29 colon cancer xenograft model^[1].
CHK1-IN-4 (10-40 mg/kg; intravenous injection; twice weekly) hydrochloride exhibits dose-dependent tumor growth inhibition in the LoVo colon cancer xenograft model^[1].

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

分子量

480.75

分子式

C₁₈H₁₉BrClN₇O₂

Appearance

Solid

SMILES

N#CC1=NC=C(NC2=NNC(C3=C(OC)C=C(Br)C=C3OCCCN)=C2)N=C1.Cl

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶剤 & 溶解度

体外:

DMSO : 5 mg/mL (10.40 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0801 mL	10.4004 mL	20.8008 mL
5 mM	0.4160 mL	2.0801 mL	4.1602 mL
10 mM	0.2080 mL	1.0400 mL	2.0801 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Xiong Cai, et al. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications. WO2017132928A1.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0801 mL	10.4004 mL	20.8008 mL	52.0021 mL
	5 mM	0.4160 mL	2.0801 mL	4.1602 mL	10.4004 mL
	10 mM	0.2080 mL	1.0400 mL	2.0801 mL	5.2002 mL