APTO-253-LOR-253-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAPTO-253Cat. No.: HY-16291CAS No.: 916151-99-0Synonyms: LOR-253; LT-253分式: CHFN分量: 367.38作靶点: KLF; G-quadruplex作通路: MAPK/ERK Pathway; Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性

2、数据体外实验 DMSO : 33.33 mg/mL (90.72 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.3 mg/mL (6.26 mM); Suspended solution; Need ultrasonic and warming2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3.03 mg/mL (8.25 mM); Suspended solution; Need ultrasonic and warmi

3、ng1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 APTO-253种 Kruppel-like factor 4 诱导剂，同时可稳定 Gquadruplex 结构，具有抗癌活性。IC50 & Target KLF4 1, Gquadruplex 3体外研究 APTO-253 is an inducer of KLF4. APTO-253 (5 M) induces KLF4 expression, and enhances apoptosisinduced by cisplatin in both

4、 SKOV3 and OVCAR3 cells. APTO-253 (5 M) also leads to G1 phase arrest andreduces S and G2/M phase cells in SKOV3 and OVCAR3 cells 1. APTO-253 is cytotoxic to Raji andRaji/253R cell lines, with IC50s of 105 2.4 nM and 1387 94 nM, respectively. APTO-253 (0.5 M) alsocauses DNA damage in Raji cells. BRC

5、A1/2 deficient cells are hypersensitive to APTO-253. ABCG2overexpressed HEK-293 cells are resistant to APTO-253 and inhibition of ABCG2 reverses resistance toAPTO-253 in Raji/253R 2. APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) celllines and various forms of lymphoma cell li

6、nes with IC50s ranging from 57 nM to 1.75 M. APTO-253 (500nM) also causes G0/G1 cell cycle arrest, induces apoptosis, and down regulates MYC RNA and proteinexpression in AML lines. APTO-253 (500 nM) leads to DNA damage response pathways in MV4-11 cells.Futhermore, APTO-253 is a potent stabilizer of

7、Gquadruplex (G4) motifs, and demonstrates the greatestpropensity for stabilizing the MYC G4 sequences 3.PROTOCOLCell Assay 3 Cells are plated and treated with vehicle DMSO or APTO-253 (10 concentrations) in 96 well plates for 5 daysat 37C and 5% CO2. Cell viability is measured using CellTiter 96 AQu

8、eous one solution cell proliferationassay, and IC50 values are calculated using GraphPad Prism 7 software 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 bioRxiv. May 30, 2018.See more customer validations on HYPERLINK / www.MedChemEREFERE

9、NCES1. Wang B, et al. KLF4 expression enhances the efficacy of chemotherapy drugs in ovarian cancer cells. Biochem Biophys Res Commun.2017 Mar 11;484(3):486-492.2. Tsai CY, et al. APTO-253 is a new addition to the repertoire of drugs that can exploit DNA BRCA1/2 deficiency. Mol Cancer Ther. 2018Apr

10、6. pii: molcanther.0834.2017.3. Local A, et al. APTO-253 stabilizes G-quadruplex DNA, inhibits MYC expression and induces DNA damage in acute myeloid leukemiacells. Mol Cancer Ther. 2018 Apr 6. pii: molcanther.1209.2017.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not been fully valid