AZD7762
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $850 | Check With Us |
500mg | $1350 | Check With Us |
1g | $2025 | Check With Us |
Cat #: V1582 CAS #: 860352-01-8 (free base) Purity ≥ 98%
Description: AZD7762 (AZD-7762; AZD 7762) is a selective and ATP-competitive inhibitor of Chk1 (checkpoint kinases) with potential anticancer activity.
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Molecular Weight (MW) | 362.42 |
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Molecular Formula | C17H19FN4O2S |
CAS No. | 860352-01-8 (free base) |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: 50 mg/mL (138.0 mM)r |
Water: <1 mg/mLr | |
Ethanol: <1 mg/mL | |
Synonyms | AZD7762; AZD 7762; AZD-7762 |
Protocol | 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 G2 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 IC50 of 5 nM as measured by a scintillation proximity assay. The Ki 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 G2 arrest induced by Camptothecin with an average EC50 of 10 nM (n=12) and maximal abrogation in the range of 100 nM |
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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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.7592 mL | 13.7961 mL | 27.5923 mL | 55.1846 mL |
5mM | 0.5518 mL | 2.7592 mL | 5.5185 mL | 11.0369 mL |
10mM | 0.2759 mL | 1.3796 mL | 2.7592 mL | 5.5185 mL |
20mM | 0.1380 mL | 0.6898 mL | 1.3796 mL | 2.7592 mL |
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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