504972 Sigma-AldrichATR Inhibitor IV - CAS 1232410-49-9 - Calbiochem
Recommended Products
Overview
| Replacement Information |
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Key Specifications Table
| CAS # | Empirical Formula |
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| 1232410-49-9 | C₁₈H₁₆N₄O₃S |
Pricing & Availability
| Catalog Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
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| 5.04972.0001 |
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Glass bottle | 10 mg |
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| Description | |
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| Overview | A cell-permeable phenylpyrazine derivative that acts as a potent, ATP-competitive (Ki= 13 nM; IC50/[ATP] = 70 nM/50 µM and 128 nM/100 µM), ATR-selective inhibitor with much reduced or little potency against 4 related PIKKs (Ki= 2.2, 3.9, 16, and >1 µM, respectively, against DNA-PK, PI 3-Kγ, ATM, and mTOR) and 50 other kinases. Shown to selectively inhibit ATR-dependent H2AX Ser139 & Chk1 Ser345 phosphorylation (complete inhibition at 10 µM in HT29 and HFL1 cultures) without affecting ATM- and DNA-PK-mediated H2AX or ATM-mediated Chk2 phosphorylation. Short-term (24 h) VE-821 treatment, either alone or in synergy with Cisplatin (Cat. No. 232120), results in reversible cytostatic growth arrest regardless of cellular ATM-p53 pathway activity, while cytotoxicity and Cisplatin synergism in cell death induction is reported to occur only upon long-term VE-821 exposure (≥72 h) in cultures with ATM-p53 pathway defects. Please note that the molecular weight for this compound is batch-specific due to variable water content. |
| Catalogue Number | 504972 |
| Brand Family | Calbiochem® |
| Synonyms | 3-amino-6-(4-(methylsulfonyl)phenyl)-N-phenylpyrazine-2-carboxamide, VE-821, ATM and Rad3-Related Inhibitor IV, VE821 |
| References | |
|---|---|
| References | Prevo, R., et al. 2012, Cancer Biol. Ther. 13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer 107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7, 428. |
| Product Information | |
|---|---|
| CAS number | 1232410-49-9 |
| Form | Yellow solid |
| Hill Formula | C₁₈H₁₆N₄O₃S |
| Chemical formula | C₁₈H₁₆N₄O₃S |
| Reversible | Y |
| Structure formula Image | |
| Quality Level | MQ100 |
| Applications |
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| Biological Information | |
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| Primary Target | ATR |
| Primary Target K<sub>i</sub> | 13nM |
| Purity | ≥98% by HPLC |
| Physicochemical Information | |
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| Cell permeable | Y |
| Dimensions |
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| Materials Information |
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| Toxicological Information |
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| Safety Information according to GHS |
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| Safety Information |
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| Product Usage Statements |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
| Transport Information |
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| Supplemental Information |
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| Specifications |
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| Global Trade Item Number | |
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| Catalog Number | GTIN |
| 5.04972.0001 | 04055977263213 |
Documentation
ATR Inhibitor IV - CAS 1232410-49-9 - Calbiochem SDS
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References
| Reference overview |
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| Prevo, R., et al. 2012, Cancer Biol. Ther. 13, 1072; Pires, I.M., et al. 2012, Br. J. Cancer 107, 291; Reaper, P.M., et al. 2011, Nat. Chem. Biol. 7, 428. |
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Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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