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APTO-253 HCl

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names：
2-(5-fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline hydrochloride
CAS號(hào)：
1691221-67-6
MDL Number：
MF(分子式)： C22H15ClFN5 MW(分子量)： 403.84
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	APTO-253 HCl
英文別名	APTO-253 hydrochloride; APTO-253 HCl; APTO 253 HCl; APTO253 HCl; LOR 253; LOR253; LOR-253; LT-253;
CAS號(hào)	1691221-67-6
Inchi	InChI=1S/C22H14FN5.ClH/c1-11-17(15-10-12(23)6-7-16(15)26-11)22-27-20-13-4-2-8-24-18(13)19-14(21(20)28-22)5-3-9-25-19;/h2-10,26H,1H3,(H,27,28);1H
InchiKey	XGEPFSYBBQZKKW-UHFFFAOYSA-N
分子式 Formula	C22H15ClFN5
分子量 Molecular Weight	403.84
溶解度Solubility
性狀	Solid powder
儲(chǔ)藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產(chǎn)品說明	APTO-253 HCl(CAS:1691221-67-6 ):僅限應(yīng)用于工業(yè)或者科學(xué)研究過程中非醫(yī)療目的，不應(yīng)用于人類或動(dòng)物的臨床診斷以及治過程療，該產(chǎn)品非藥用，非食用。
Introduction	APTO-253, also known as LOR-253, LT-253, is a small molecule inhibitor of human metal-regulatory transcription factor 1 (MTF-1) with potential antitumor activity. MTF-1 inhibitor LOR-253 inhibits MTF-1 activity and thereby induces the expression of MTF-1 dependent tumor suppressor factor Kruppel like factor 4 (KLF4). This subsequently leads to the downregulation of cyclin D1, blocking cell cycle progression and proliferation. This agent also causes decreased expression of genes involved in tumor hypoxia and angiogenesis.
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[1]Local A, Zhang H, Benbatoul KD, Folger P, Sheng X, Tsai CY, Howell SB, Rice WG. APTO-253 Stabilizes G-quadruplex DNA, Inhibits MYC Expression, and Induces DNA Damage in Acute Myeloid Leukemia Cells. Mol Cancer Ther. 2018 Jun;17(6):1177-1186. doi: 10.1158/1535-7163.MCT-17-1209. Epub 2018 Apr 6. PubMed PMID: 29626127.

[2]Tsai CY, Sun S, Zhang H, Local A, Su Y, Gross LA, Rice WG, Howell SB. APTO-253 Is a New Addition to the Repertoire of Drugs that Can Exploit DNA BRCA1/2 Deficiency. Mol Cancer Ther. 2018 Jun;17(6):1167-1176. doi: 10.1158/1535-7163.MCT-17-0834. Epub 2018 Apr 6. PubMed PMID: 29626126.

[3] Wang B, Shen A, Ouyang X, Zhao G, Du Z, Huo W, Zhang T, Wang Y, Yang C, Dong P, Watari H, Pfeffer LM, Yue J. KLF4 expression enhances the efficacy of chemotherapy drugs in ovarian cancer cells. Biochem Biophys Res Commun. 2017 Mar 11;484(3):486-492. doi: 10.1016/j.bbrc.2017.01.062. Epub 2017 Jan 18. PubMed PMID: 28108288.

[4] Cercek A, Wheler J, Murray PE, Zhou S, Saltz L. Phase 1 study of APTO-253 HCl, an inducer of KLF4, in patients with advanced or metastatic solid tumors. Invest New Drugs. 2015 Oct;33(5):1086-92. doi: 10.1007/s10637-015-0273-z. Epub 2015 Aug 14. PubMed PMID: 26268924.

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