WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 599220
CAS#: 1691221-67-6 (HCl)
Description: 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.
MedKoo Cat#: 599220
Name: APTO-253 HCl
CAS#: 1691221-67-6 (HCl)
Chemical Formula: C22H15ClFN5
Molecular Weight: 403.84
Elemental Analysis: C, 65.43; H, 3.74; Cl, 8.78; F, 4.70; N, 17.34
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Synonym: APTO-253 hydrochloride; APTO-253 HCl; APTO 253 HCl; APTO253 HCl; LOR 253; LOR253; LOR-253; LT-253;
IUPAC/Chemical Name: 2-(5-fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline hydrochloride
InChi Key: XGEPFSYBBQZKKW-UHFFFAOYSA-N
InChi Code: 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
SMILES Code: CC(N1)=C(C2=NC3=C4C=CC=NC4=C5N=CC=CC5=C3N2)C6=C1C=CC(F)=C6.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 403.84 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
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.