1204956-74-0
Chemical Structure
COTI-2 hydrochloride
- CAS No.: 1204956-74-0
- Formula:C19H23ClN6S
- Molecular Weight:402.94
InChIKey: AJEFZRURUAFCRQ-YHLMHSEJSA-N
SMILES: S=C(N1CCN(CC1)C2=NC=CC=C2)N/N=C3C4=NC=CC=C4CCC/3.Cl
Biological Activity: COTI-2 hydrochloride is an orally active thiosemicarbazone anticancer agent and p53 mutant activator. COTI-2 hydrochloride induces Apoptosis. COTI-2 hydrochloride triggers the activation of AMPK and the inhibition of the mTOR pathway. COTI-2 hydrochloride induces DNA damage and replication stress responses. COTI-2 hydrochloride binds to misfolded mutant p53 proteins, thereby inducing conformational changes that restore p53 to its normal state and reactivate its function. COTI-2 hydrochloride acts on a variety of cancer cell lines and xenografts. COTI-2 hydrochloride can be used in research related to colorectal cancer, small cell lung cancer, glioblastoma, breast cancer, and ovarian cancer[1][2][3].
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COTI-2 hydrochloride | COTI-2 hydrochloride is an orally active thiosemicarbazone anticancer agent and p53 mutant activator. COTI-2 hydrochloride induces Apoptosis. COTI-2 hydrochloride triggers the activation of AMPK and the inhibition of the mTOR pathway. COTI-2 hydrochloride induces DNA damage and replication stress responses. COTI-2 hydrochloride binds to misfolded mutant p53 proteins, thereby inducing conformational changes that restore p53 to its normal state and reactivate its function. COTI-2 hydrochloride acts on a variety of cancer cell lines and xenografts. COTI-2 hydrochloride can be used in research related to colorectal cancer, small cell lung cancer, glioblastoma, breast cancer, and ovarian cancer. | |||||||||||||||||||||
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- [1]. Salim KY, et al. COTI-2, a novel small molecule that is active against multiple human cancer cell lines in vitro and in vivo. Oncotarget. 2016 Jul 05;7(27):41363-41379. [Content Brief]
- [2]. Duffy MJ, et al. Mutant p53 as a target for cancer treatment. Eur J Cancer. 2017 Sep;83:258-265. [Content Brief]
- [3]. Lindemann A, et al. COTI-2, A Novel Thiosemicarbazone Derivative, Exhibits Antitumor Activity in HNSCC through p53-dependent and -independent Mechanisms. Clin Cancer Res. 2019 Sep 15;25(18):5650-5662. [Content Brief]
Keywords
