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Navitoclax

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产品编号 T2101Cas号 923564-51-6
别名 ABT-263

Navitoclax (ABT-263) 是一种 Bcl-2 抑制剂,可与 Bcl-xL、Bcl-2、Bcl-w 等蛋白结合 (Ki<1 nM),具有有效性和口服活性。Navitoclax 具有抗肿瘤活性,可以诱导细胞凋亡。

Navitoclax

Navitoclax

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纯度: 100%
产品编号 T2101 别名 ABT-263Cas号 923564-51-6

Navitoclax (ABT-263) 是一种 Bcl-2 抑制剂,可与 Bcl-xL、Bcl-2、Bcl-w 等蛋白结合 (Ki<1 nM),具有有效性和口服活性。Navitoclax 具有抗肿瘤活性,可以诱导细胞凋亡。

规格价格库存数量
1 mg¥ 233现货
5 mg¥ 535现货
10 mg¥ 797现货
25 mg¥ 1,370现货
50 mg¥ 1,980现货
100 mg¥ 2,890现货
200 mg¥ 3,960现货
500 mg¥ 5,820现货
1 g¥ 7,860现货
1 mL x 10 mM (in DMSO)¥ 659现货
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产品介绍

生物活性
产品描述
Navitoclax (ABT-263) is a Bcl-2 inhibitor that binds to Bcl-xL, Bcl-2, and Bcl-w proteins (Ki<1 nM) with potent and oral activity. Navitoclax has antitumor activity and induces apoptosis.
靶点活性
BCL-XL:0.4 nM (Ki, cell free), BCL2:<1 nM (Ki, cell free), BCL-W:<1 nM (Ki, cell free)
体外活性
方法:鼠原 B 淋巴细胞 FL5.12/Bcl-xL 和 FL5.12/Bcl-2 用 Navitoclax (0.001-1000 nmol/L) 处理 48 h,使用 CellTiter Glo 方法检测细胞活力。
结果:Navitoclax 逆转了 Bcl-2 或 Bcl-xL 的过表达所提供的保护 (EC50 分别为 60 和 20 nmol/L)。在 IL-3 存在的情况下,在 FL5.12 细胞不受促凋亡刺激的情况下,Navitoclax 诱导细胞死亡是无效的。[1]
方法:HCC 细胞 PLC/PRF/5、Hep3B、HepG2 和 Huh7 用 Navitoclax (5 μM) 处理 18 h,使用 Western Blot 方法检测靶点蛋白表达水平。
结果:在用 Navitoclax 治疗后,所有 HCC 细胞系中的 Mcl-1 水平显著增加,但 Bcl-2 和B cl-xL 水平没有显著变化。[2]
体内活性
方法:为检测体内抗肿瘤活性,将 Navitoclax (100 mg/kg in 10% ethanol+30% polyethylene glycol 400+60% Phosal 50 PG) 口服给药给携带人 SCLC 和 ALL 异种移植物的 scid 小鼠,每天一次,持续二十一天。
结果:口服 Navitoclax 导致体内 SCLC 和 ALL 异种移植物肿瘤消退。[1]
方法:为检测体内抗肿瘤活性,将 Navitoclax (50-100 mg/kg in 10% ethanol+30% polyethylene glycol 400+60% Phosal 50 PG) 单剂量口服给药给携带人 SCLC 肿瘤 H146 的 scid 小鼠。
结果:单剂量 Navitoclax 治疗的 H146 肿瘤显示出大量的死亡和垂死细胞,包括血管化良好的肿瘤周围。[3]
激酶实验
ABT-737 and ABT-263 were synthesized as previously described. The enantiomer and BH3-only peptides were synthesized at Abbott. Binding affinities (Ki or IC50) were determined with competitive fluorescence polarization assays. The following peptide probe/protein pairs were used: f-bad (1 nmol/L) and Bcl-xL (6 nmol/L), f-Bax (1 nmol/L) and Bcl-2 (10 nmol/L), f-Bax (1 nmol/L) and Bcl-w (40 nmol/L), f-Noxa (2 nmol/L) and Mcl-1 (40 nmol/L), and f-Bax (1 nmol/L) and Bcl-2-A1 (15 nmol/L). Binding affinities for Bcl-xL were also determined using a time-resolved fluorescence resonance energy transfer assay. Bcl-xL (1 nmol/L, His tagged) was mixed with 200 nmol/L f-Bak, 1 nmol/L Tb-labeled anti-His antibody, and compound at room temperature for 30 min. Fluorescence was measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-His antibody) emission filters. Dissociation constants (Ki) were determined using Wang's equation [1].
细胞实验
Human tumor cell lines were maintained at 37°C containing 5% CO2. SCLC cell lines were cultured in RPMI 1640 with 10% fetal bovine serum (FBS), 1% sodium pyruvate, 25 mmol/L HEPES, 4.5 g/L glucose, and 1% penicillin/streptomycin. Leukemia and lymphoma cell lines were cultured in RPMI 1640 supplemented with 10% FBS and 1% penicillin/streptomycin. Cells (1 × 10^4–5 × 10^4) were treated for 48 h in 96-well culture plates in a final volume of 100 μL and cytotoxicity was assessed with the CellTiter Glo assay [1].
动物实验
C.B.-17 scid-bg or C.B.-17 scid mice were implanted with 5 × 10^6 (1 × 10^6 for DoHH2) cells in 0.2 mL 50% Matrigel s.c. into the right flank. Tumor-bearing mice were size matched (~235 mm3; day 0) into treatment and control groups, ear tagged, and monitored individually. Tumor volume was measured two to three times weekly by electronic calipers (volume = length × width2 / 2). Tumor growth inhibition was calculated based on the difference in mean tumor volumes between treated and appropriate vehicle control groups. Partial response (PR) is defined as ≥50% tumor growth inhibition, and complete response (CR) is defined as nonpalpable tumor. All studies used 8 to 10 mice per group. ABT-263 was formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG and administered p.o. The other agents used [rituximab, doxorubicin, cyclophosphamide, vincristine, bortezomib, and prednisone] were administered i.p., p.o., or i.v. and formulated according to the manufacturers' recommendations. For combination studies, ABT-263 was given ~2 h before the other agents, except bortezomib, which was given ~4 h before ABT-263 [1].
别名ABT-263
化学信息
分子量974.61
分子式C47H55ClF3N5O6S3
CAS No.923564-51-6
SmilesC(C1=C(CCC(C)(C)C1)C2=CC=C(Cl)C=C2)N3CCN(CC3)C4=CC=C(C(NS(=O)(=O)C5=CC(S(C(F)(F)F)(=O)=O)=C(N[C@H](CCN6CCOCC6)CSC7=CC=CC=C7)C=C5)=O)C=C4
密度1.41 g/cm3
储存&溶解度
存储store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 50 mg/mL (51.3 mM), Sonication is recommended.
H2O: < 1 mg/mL (insoluble or slightly soluble)
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM1.0261 mL5.1303 mL10.2605 mL51.3026 mL
5 mM0.2052 mL1.0261 mL2.0521 mL10.2605 mL
10 mM0.1026 mL0.5130 mL1.0261 mL5.1303 mL
20 mM0.0513 mL0.2565 mL0.5130 mL2.5651 mL
50 mM0.0205 mL0.1026 mL0.2052 mL1.0261 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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%Tween 80
%ddH2O

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