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AZD7762 hydrochloride

Cat. No. M3686
AZD7762 hydrochloride Structure
Synonym:

AZD-7762 HCl

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 90  USD90 In stock
5mg USD 80  USD80 In stock
10mg USD 125  USD125 In stock
50mg USD 390  USD390 In stock
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Quality Control
Biological Activity

AZD7762 hydrochloride is a potent ATP-competitive checkpoint kinase inhibitor with an IC50 of 5 and <10 nM for CHK1 and CHK2 respectively. AZD7762 has been profiled extensively in vitro andin vivo in combination with DNA-damaging agents and has been shown to potentiate response in several different settings where inhibition of checkpoint kinase results in the abrogation of DNA damage-induced cell cycle arrest.

Customer Product Validations & Biological Datas
Source J Natl Cancer Inst (2017). Figure 3. AZD7762
Method Effects of carbamoyl phosphate synthetase 1 (CPS1) knockdown
Cell Lines LKB1-intact cell line
Concentrations 10 μM
Incubation Time -
Results We examined the effects of CPS1 knockdown combined with gemcitabine and pemetrexed, which interfere with DNA synthesis pathways and are frequently used to treat LADC, as well as with CHK1 inhibitor AZD7762, to which LKB1-deficient lung cancer was recently shown to be sensitive
Protocol
Cell Experiment
Cell lines SW620 and MDA-MB-231 cells line
Preparation method Potentiation Assays.
SW620 (5.5 × 103 per well) or MDA-MB-231 (5 × 103 per well) cells were seeded in 96-well plates and incubated overnight. Cells were dosed for 24 h with a 9-point titration of gemcitabine ranging from 0.01 to 100 nmol/L with or without a constant dose of AZD7762 (300 nmol/L). Control wells were dosed with vehicle alone (0.1% DMSO) or 300 nmol/L AZD7762. After 24 h, medium was removed and AZD7762 alone was added back to the wells treated previously with AZD7762 for an additional 24 h. Cells were then incubated in drug-free medium for an additional 72 h. The effect on cell proliferation was determined by 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethophenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt assay as recommended by the supplier (Promega). The same experimental procedure was used for topotecan combinations (topoisomerase I inhibitor, analogue of camptothecin) except an 11-point titration of topotecan ranging from 0.1 nmol/L to 30 μmol/L was used. Net growth was calculated (AT120 - AT0 / predose) × 100 and plotted versus concentration of chemotherapy in the presence and absence of AZD7762. IC50 values were calculated by concentration-response fitting using four-variable logistical equations (Sigmoidal fit) within Origin Pro.
Concentrations 0.01 ~ 100 nmol/L
Incubation time 48 h
Animal Experiment
Animal models Xenograft Models in Mice
Formulation 11.3% hydroxyproplyl-β-cyclodextrin
Dosages 50~100mg/kg every 3 days
Administration i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 398.88
Formula C17H19FN4O2S.HCl
CAS Number 1246094-78-9
Purity 100.00%
Solubility DMSO 15 mg/mL
Storage at -20°C
References

[1] Ma, et al. Mol Med Report. The Chk1 inhibitor AZD7762 sensitises p53 mutant breast cancer cells to radiation in vitro and in vivo.

[2] Landau, et al. Mol Cancer Ther. The Checkpoint Kinase Inhibitor AZD7762 Potentiates Chemotherapy-Induced Apoptosis of p53-Mutated Multiple Myeloma Cells.

[3] Oza, et al. J Med Chem. Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.

[4] Aris, et al. Cancer Res. Potentiation of the novel topoisomerase I inhibitor indenoisoquinoline LMP-400 by the cell checkpoint and Chk1-Chk2 inhibitor AZD7762.

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Keywords: AZD7762 hydrochloride, AZD-7762 HCl supplier, Checkpoint, inhibitors

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