[CAS NO. 860352-01-8] AZD-7762

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PRODUCTS SPECIFICATIONS [860352-01-8]

Catelog

HY-10992

Brand

MCE

CAS

860352-01-8

DESCRIPTION [860352-01-8]

Overview

MDL	MFCD12406007
Molecular Weight	362.42
Molecular Formula	C17H19FN4O2S
SMILES	O=C(N[C@@H]1CNCCC1)C2=C(C=C(S2)C3=CC=CC(F)=C3)NC(N)=O

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

15 Publications Citing Use of MCE

Summary

AZD-7762 is a potent ATP-competitive checkpoint kinase ( Chk ) inhibitor in with an IC ₅₀ of 5 nM for Chk1 .

IC50 & Target

Chk1

5 nM (IC ₅₀ )

Chk2

5 nM (IC ₅₀ )

In Vitro

AZD-7762 (AZD7762) is an equally potent inhibitor of Chk1 and Chk2 in vitro. AZD-7762 potently inhibits Chk1 and Chk2, abrogates DNA damage-induced S and G ₂ checkpoints, enhances the efficacy of NSC 613327 and SKF 104864A, and modulates downstream checkpoint pathway proteins. AZD-7762 potently inhibits Chk1 phosphorylation of a cdc25C peptide with an IC ₅₀ of 5 nM as measured by a scintillation proximity assay. The K _i for AZD-7762 is determined to be 3.6 nM. Kinetic characterization suggests that AZD-7762 binds in the ATP-binding site of Chk1 and is thought to compete directly for ATP binding in a reversible manner. AZD-7762 is shown to abrogate the G ₂ arrest induced by Camptothecin with an average EC ₅₀ of 10 nM (n=12) and maximal abrogation in the range of 100 nM ^[1] .

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

In Vivo

In the rat H460-DNp53 xenograft study, AZD-7762 (AZD7762) potentiates the antitumor activity of NSC 613327 in a dose-dependent manner by a decrease in %T/C with increasing dose (48% and 32%, 10 and 20 mg/kg AZD-7762, respectively). In the mouse xenograft study in combination with CPT-11, SW620 established tumors are treated with vehicle, CPT-11 alone, AZD-7762 alone, or AZD-7762 in combination with CPT-11. AZD-7762 dosed alone shows insignificant antitumor activity, whereas CPT-11 alone displays striking and significant activity (%T/C with increasing dose is 9 and 1, respectively ). In combination with AZD-7762, %T/C increases significantly to -66% and -67%, respectively ^[1] . AZD7762 combination with CX-5461 induces cancer cell death of Tp53 -null ( Tp53 ^-/- ) Eμ- Myc lymphoma cells in vitro and in vivo ^[2] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00413686	AstraZeneca	Solid Tumors	December 2006	Phase 1
NCT00937664	AstraZeneca	Cancer\|Solid Tumors\|Advanced Solid Malignancies	July 2009	Phase 1
NCT00473616	AstraZeneca	Advanced Solid Tumors\|Cancer\|Advanced Solid Malignancies	May 2007	Phase 1

Appearance

Solid

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 : 100 mg/mL ( 275.92 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7592 mL	13.7961 mL	27.5923 mL
5 mM	0.5518 mL	2.7592 mL	5.5185 mL
10 mM	0.2759 mL	1.3796 mL	2.7592 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% HP-β-CD

Solubility: 10 mg/mL (27.59 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

2-Thiophenecarboxamide, 3-[(aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-

3-[(Aminocarbonyl)amino]-5-(3-fluorophenyl)-N-(3S)-3-piperidinyl-2-thiophenecarboxamide

5-(3-Fluorophenyl)-3-ureidothiophene-2-carboxylic acid N-[(S)-piperidin-3-yl]amide

AZD 7762