货号	规格	价格	上海	北京	珠海	重庆	武汉
S87245-5mg买3赠1	99.70%	￥480.00 S87245-5mg ￥480.00 现货（买3赠1）	5 5	-	-	-	-
S87245-10mg买3赠1	99.70%	￥670.00 S87245-10mg ￥670.00 现货（买3赠1）	7 7	-	-	-	-
S87245-50mg买3赠1	99.70%	￥1800.00 S87245-50mg ￥1800.00 现货（买3赠1）	3 3	-	-	-	-
S87245-100mg	≥99%	￥2900.00 S87245-100mg ￥2900.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

APTO-253 (LOR-253) is a small molecule that inhibits c-Myc expression, stabilizes G-quadruplex DNA, and induces cell cycle arrest and apoptosis in acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of the Krüppel-like factor 4 (KLF4) tumor suppressor. APTO-253 has antiarthritic activity

靶点：

c-Myc; KLF4;Apoptosis;c-Myc;KLF

体外研究：

APTO-253 is an inducer of KLF4. APTO-253 (5 μM) induces KLF4 expression, and enhances apoptosis induced by NSC 119875 in both SKOV3 and OVCAR3 cells. APTO-253 (5 μM) also leads to G1 phase arrest and reduces S and G2/M phase cells in SKOV3 and OVCAR3 cells.
APTO-253 is cytotoxic to Raji and Raji/253R cell lines, with IC50s of 105 ± 2.4 nM and 1387 ± 94 nM, respectively. APTO-253 (0.5 μM) also causes DNA damage in Raji cells. BRCA1/2 deficient cells are hypersensitive to APTO-253. ABCG2 overexpressed HEK-293 cells are resistant to APTO-253 and inhibition of ABCG2 reverses resistance to APTO-253 in Raji/253R.
APTO-253 suppresses the proliferation of acute myeloid leukemia (AML) cell lines and various forms of lymphoma cell lines with IC50s ranging from 57 nM to 1.75 µM. APTO-253 (500 nM) also causes G0/G1 cell cycle arrest, induces apoptosis, and down regulates MYC RNA and protein expression 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 Gquadruplex (G4) motifs, and demonstrates the greatest propensity for stabilizing the MYC G4 sequences.

体内研究：

APTO-253 (LOR-253; 15 mg/kg; IV; twice per day for 2 consecutive days per week for 14 days) has antiarthritic activity in a CIA model. Animal Model: DBA/1J male mice (6 weeks) with collagen induced arthritis (CIA) Dosage: 15 mg/kg Administration: IV; twice per day for 2 consecutive days per week for 14 days Result: Demonstrated significant preventive and therapeutic activity on arthritis formation.

参考文献：

1. Local A, et al. 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. 2. Hongying Zhang, et al. Inhibition of c-Myc By Apto-253 As an Innovative Therapeutic Approach to Induce Cell Cycle Arrest and Apoptosis in Acute Myeloid Leukemia. Blood 2016 128:1716. 3. Haruka Tsuchiya, et al. Parsing multiomics landscape of activated synovial fibroblasts highlights drug targets linked to genetic risk of rheumatoid arthritis. Ann Rheum Dis. 2020 Nov2;annrheumdis-2020-218189.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.722 ml	13.61 ml	27.22 ml
5 mM	0.544 ml	2.722 ml	5.444 ml
10 mM	0.272 ml	1.361 ml	2.722 ml
50 mM	0.054 ml	0.272 ml	0.544 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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LOR 253