AZD-7762 hydrochloride

Name: AZD-7762 hydrochloride
Brand: MedChemExpress
SKU: HY-10992A
Rating: 5.0 (23 reviews)

Cat. No.: HY-10992A Purity: 99.58%: FAQs
Data Sheet SDS COA Handling Instructions Technical Support

AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC₅₀ of 5 nM for Chk1.

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

AZD-7762 hydrochloride Chemical Structure

CAS No. : 1246094-78-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 23 publication(s) in Google Scholar

Other Forms of AZD-7762 hydrochloride:

AZD-7762 In-stock

22 Publications Citing Use of MCE AZD-7762 hydrochloride

: AZD-7762 hydrochloride purchased from MedChemExpress. Usage Cited in: PLoS One. 2017 Jan 18;12(1):e0170308. [Abstract]; Inhibition of nuclear actin filament formation by Chek1/2 inhibitor, AZD7762 (AZD). No nuclear actin filament formation is observed upon treatment of CEOs with AZD alone.

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View All Checkpoint Kinase (Chk) Isoform Specific Products:

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Chk1 Chk2

Biological Activity
Purity & Documentation
References
Customer Review

Description

AZD-7762 hydrochloride is a potent ATP-competitive checkpoint kinase (Chk) inhibitor in with an IC₅₀ of 5 nM for Chk1.

IC₅₀ & Target^[1]

Chk1

5 nM (IC₅₀)

Chk2

5 nM (IC₅₀)

In Vitro

AZD-7762 hydrochloride (AZD7762) is an equally potent inhibitor of Chk1 and Chk2 in vitro. AZD-7762 hydrochloride potently inhibits Chk1 and Chk2, abrogates DNA damage-induced S and G₂ checkpoints, enhances the efficacy of NSC 613327 and SKF 104864A, and modulates downstream checkpoint pathway proteins. AZD-7762 hydrochloride potently inhibits Chk1 phosphorylation of a cdc25C peptide with an IC₅₀ of 5 nM as measured by a scintillation proximity assay. The K_i for AZD-7762 hydrochloride is determined to be 3.6 nM. Kinetic characterization suggests that AZD-7762 hydrochloride binds in the ATP-binding site of Chk1 and is thought to compete directly for ATP binding in a reversible manner. AZD-7762 hydrochloride is shown to abrogate the G₂ arrest induced by Camptothecin with an average EC₅₀ of 10 nM (n=12) and maximal abrogation in the range of 100 nM^[1].

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

In Vivo

In rat H460-DNp53 xenograft studies, AZD-7762 hydrochloride (10 mg/kg and 20 mg/kg) potentiates the antitumor activity of NSC 613327 in a dose-dependent manner. That is, the inhibition rate (%T/C) decreases to 48% and 32%, respectively, with increasing dose. In a mouse xenograft study in combination with CPT-11, treatment with AZD-7762 hydrochloride in combination with CPT-11 significantly increased CPT-11 activity with a significant increase in %T/C to -66% and -67%, respectively^[1]. AZD7762 hydrochloride in combination with CX-5461 induces Tp53-null (Tp53^-/-) Eμ-Myc in vitro and in vivo Lymphoma cell death^[2].

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

Clinical Trial

Molecular Weight

398.88

Formula

C₁₇H₂₀ClFN₄O₂S

CAS No.

1246094-78-9

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(NC(N)=O)C=C(C2=CC=CC(F)=C2)S1)N[C@@H]3CNCCC3.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 20 mg/mL (50.14 mM; ultrasonic and warming and heat to 60°C; 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	2.5070 mL	12.5351 mL	25.0702 mL
5 mM	0.5014 mL	2.5070 mL	5.0140 mL
10 mM	0.2507 mL	1.2535 mL	2.5070 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)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2 mg/mL (5.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (5.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.58%

Select Batch:

Data Sheet (280 KB) SDS (614 KB)

COA (257 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Zabludoff SD, et al. AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies. Mol Cancer Ther. 2008 Sep;7(9):2955-66. [Content Brief]

[2]. Quin J, et al. Inhibition of RNA polymerase I transcription initiation by CX-5461 activates non-canonical ATM/ATR signaling. Oncotarget. 2016 Aug 2;7(31):49800-49818. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5070 mL	12.5351 mL	25.0702 mL	62.6755 mL
	5 mM	0.5014 mL	2.5070 mL	5.0140 mL	12.5351 mL
	10 mM	0.2507 mL	1.2535 mL	2.5070 mL	6.2675 mL
	15 mM	0.1671 mL	0.8357 mL	1.6713 mL	4.1784 mL
	20 mM	0.1254 mL	0.6268 mL	1.2535 mL	3.1338 mL
	25 mM	0.1003 mL	0.5014 mL	1.0028 mL	2.5070 mL
	30 mM	0.0836 mL	0.4178 mL	0.8357 mL	2.0892 mL
	40 mM	0.0627 mL	0.3134 mL	0.6268 mL	1.5669 mL
	50 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2535 mL