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Formula | C17H19N5OS |
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Molecular Weight | 341.43 | CAS No. | 1330782-76-7 | |
Solubility (25°C)* | In vitro | DMSO | 68 mg/mL (199.16 mM) | |
Ethanol | 4 mg/mL (11.71 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Simurosertib (TAK-931), an oral cell division cycle 7 (CDC7)-selective inhibitor with an IC50<0.3 nM, induces S phase delay and replication stress and causes mitotic aberrations through centrosome dysregulation and chromosome missegregation, resulting in irreversible antiproliferative effects in cancer cells. | ||
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In vitro | Simurosertib (TAK-931) induces S phase delay and Replication stress (RS). Simurosertib-induced RS causes mitotic aberrations through centrosome dysregulation and chromosome missegregation, resulting in irreversible antiproliferative effects in cancer cells.<sup><a class="sref" href="#s_ref">[1]</a></sup> |
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In vivo | Simurosertib (TAK-931) has marked, dose-dependent antitumor activity, without severe body weight loss in the pancreatic cancer cell (COLO205 and SW948) xenograft models.<sup><a class="sref" href="#s_ref">[1]</a></sup> |
Description | Simurosertib (TAK-931), an oral cell division cycle 7 (CDC7)-selective inhibitor with an IC50<0.3 nM, induces S phase delay and replication stress and causes mitotic aberrations through centrosome dysregulation and chromosome missegregation, resulting in irreversible antiproliferative effects in cancer cells. | ||
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Targets |
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Cancer-associated FBXW7 loss is synthetic lethal with pharmacological targeting of CDC7 [ Mol Oncol, 2023, 10.1002/1878-0261.13537] | PubMed: 37866880 |
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SHIPPING AND STORAGE
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