化合物 Navitoclax|T2101|TargetMol

Navitoclax
923564-51-6

￥233 1mg 起订

￥535 5mg 起订

￥797 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 Navitoclax

英文名称：: Navitoclax

CAS号：: 923564-51-6

品牌：: TargetMol

产地：: 美国

保存条件：: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.67%

产品类别：: 抑制剂

货号：: T2101

Product Introduction

Bioactivity

名称	Navitoclax
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.
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].
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].
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].
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]
存储条件	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	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)
关键字	inhibit \| Inhibitor \| Bcl-2 Family \| Navitoclax \| ABT 263 \| ABT263
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ABT-263|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子