SAR-020106

Cat. No.: HY-100195 Purity: 98.04%: FAQs
Data Sheet SDS COA Handling Instructions

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SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC₅₀ of 13.3 nM for human CHK1. SAR-020106 shows excellent selectivity over CHK2. SAR-020106 significantly enhances the cell killing of Gemcitabine and SN38 by 3- to 29-fold in several colon tumor lines and in a p53-dependent fashion. SAR-020106 can enhance antitumor activity with selected anticancer agents.

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

SAR-020106 Chemical Structure

CAS No. : 1184843-57-9

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 143	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 143	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 670	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Biological Activity
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Description

In Vitro

SAR-020106 (0.1-1 μM; 23 hours) abrogates an Etoposide-induced S and G2 arrest^[1].
SAR-020106 is capable of abrogating Etoposide-induced cell cycle arrest with an IC₅₀ of 55 nM and 91 nM in HT29 and SW620 cells, respectively. SAR-020106 is relatively nontoxic with a GI₅₀ of 0.48 μM in HT29 and 2 μM in SW620, resulting in an activity index of 8.7 and 22, respectively. SAR-020106 inhibits cytotoxic drug-induced autophosphorylation of CHK1 at S296 and blocks the phosphorylation of CDK1 at Y15 in a dose-dependent fashion^[1].

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

In Vivo

SAR-020106 (40 mg/kg; i.p.; administered on days 0, 1, 7, 8, 14, and 15) in combination with Irinotecan potentiates the antitumor activity in SW620 xenografts^[1].

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

Animal Model:	Nude mice bearing SW620 xenograft tumors^[1]
Dosage:	40 mg/kg
Administration:	I.p.; administered on days 0, 1, 7, 8, 14, and 15
Result:	There was a clear decrease in tumor growth associated with the combination with tumors reaching 300% by 12.5 days.

Molecular Weight

382.85

Formula

C₁₉H₁₉ClN₆O

CAS No.

1184843-57-9

Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1=NC=C(NC2=CC3=C(C=N2)C(Cl)=CC=C3)N=C1O[C@H](C)CN(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (13.06 mM; Need ultrasonic; 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	2.6120 mL	13.0599 mL	26.1199 mL
5 mM	0.5224 mL	2.6120 mL	5.2240 mL
10 mM	0.2612 mL	1.3060 mL	2.6120 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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

Purity & Documentation

Purity: 98.04%

Select Batch:

Data Sheet (246 KB) SDS (0 KB)

COA (246 KB) RP-HPLC (249 KB)

Handling Instructions (2659 KB)

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.6120 mL	13.0599 mL	26.1199 mL	65.2997 mL
	5 mM	0.5224 mL	2.6120 mL	5.2240 mL	13.0599 mL
	10 mM	0.2612 mL	1.3060 mL	2.6120 mL	6.5300 mL

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:

SAR-0201061184843-57-9SAR020106SAR 020106Inhibitorinhibitorinhibit

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