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APTO-253
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
APTO-253图片
CAS NO:916151-99-0
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
LOR-253
LT-253
产品介绍
APTO-253 (LOR-253) 是一种小分子,可抑制c-Myc表达,稳定 G-四链体 DNA 并诱导急性髓样白血病细胞的细胞周期停滞和凋亡。APTO-253 通过诱导 Kruppel-like factor 4(KLF4)抑癌因子介导抗癌活性。APTO-253 具有抗关节炎活性。
生物活性

APTO-253 (LOR-253) is a small molecule that inhibitsc-Mycexpression, stabilizesG-quadruplexDNA, and induces cell cycle arrest andapoptosisin acute myeloid leukemia cells. APTO-253 mediates anticancer activity through induction of theKrüppel-like factor 4 (KLF4)tumor suppressor[1][2]. APTO-253 has antiarthritic activity[3].

IC50& Target

c-Myc[1]; KLF4[2]

体外研究
(In Vitro)

APTO-253 (LOR-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[1].
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[2].
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[3].

体内研究
(In Vivo)

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[3].

Animal Model:DBA/1J male mice (6 weeks) with collagen induced arthritis (CIA)[3]
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.
Clinical Trial
分子量

367.38

性状

Solid

Formula

C22H14FN5

CAS 号

916151-99-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 60 mg/mL(163.32 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.7220 mL13.6099 mL27.2198 mL
5 mM0.5444 mL2.7220 mL5.4440 mL
10 mM0.2722 mL1.3610 mL2.7220 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: 2.3 mg/mL (6.26 mM); Suspended solution; Need ultrasonic and warming

    此方案可获得 2.3 mg/mL (6.26 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 23.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: 2.08 mg/mL (5.66 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (5.66 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。