Home Cell Cycle CDK inhibitor Simurosertib For research use only.

Simurosertib

Synonyms: TAK-931

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.

Simurosertib Chemical Structure

Simurosertib Chemical Structure

CAS: 1330782-76-7

Selleck's Simurosertib has been cited by 1 publication

Purity & Quality Control

Batch: S892501 DMSO] 68 mg/mL] false] Ethanol] 4 mg/mL] false] Water] Insoluble] false Purity: 99.79%
99.79

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Signaling Pathway

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CDK Signaling Pathway

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Biological Activity

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.
Targets
Cdc7 [1]
(in CDC7 enzyme assay)
0.3 nM
In vitro
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>
Cell Research Cell lines COLO205, SW948
Concentrations 0.01-3 mM
Incubation Time 72 h
Method

Simurosertib is added 24 hours after cell seeding. After a 72-hour incubation with Simurosertib, cells are fixed and stained with nuclear dye and fluorescently labeled pHH3 to allow visualization of nuclei and mitotic cells.
In Vivo
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>
Animal Research Animal Models COLO205 and SW948 xenograft models (BALB/c nude mice)
Dosages 60 mg/kg, 80 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03708211 Completed
Neoplasms Advanced Solid
Millennium Pharmaceuticals Inc.|Takeda
 March 28 2019 Phase 1
NCT03261947 Completed
Metastatic Pancreatic Cancer|Colorectal Cancer|Esophageal Neoplasms|Carcinoma Non-small-cell Lung
Millennium Pharmaceuticals Inc.|Takeda
 October 25 2017 Phase 2
NCT02699749 Completed
Nonhematologic Neoplasms Advanced
Millennium Pharmaceuticals Inc.|Takeda
 March 24 2016 Phase 1

Chemical Information & Solubility

Molecular Weight 341.43 Formula

C17H19N5OS
CAS No. 1330782-76-7 SDF --
Smiles CC1=C(C=NN1)C2=CC3=C(S2)C(=O)NC(=N3)C4CC5CCN4CC5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 68 mg/mL ( (199.16 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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