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Navitoclax

产品编号 T2101 CAS 923564-51-6

别名: ABT-263

Navitoclax 是有效，可口服的Bcl-2抑制剂，可与Bcl-xL，Bcl-2， Bcl-w 等多种Bcl-2家族蛋白结合，Ki 值小于 1 nM。

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Navitoclax, CAS 923564-51-6

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选择批次

纯度: 100%

纯度: 99.67%

纯度: 99.43%

纯度: 99.22%

纯度: 99%

纯度: 98.88%

纯度: 98.65%

纯度: 98.46%

纯度: 98.13%

纯度: 98%

纯度: 95.82%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Navitoclax (ABT-263) is a potent, orally bioavailable Bcl-2 family protein inhibitor that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki < 1 nM for all three proteins).
靶点活性	Bcl-W:<1 nM (Ki, cell free), Bcl-xL:0.4 nM (Ki, cell free), Bcl-2:<1 nM (Ki, cell free)
体外活性	ABT-263 is a potent, orally bioavailable Bad-like BH3 mimetic (K(i)'s of <1 nmol/L for Bcl-2, Bcl-xL, and Bcl-w). In human tumor cells, ABT-263 induces Bax translocation, cytochrome c release, and subsequent apoptosis [1]. ABT-263 was active against approximately one-half of the cell lines of the PPTP in vitro panel [2].
体内活性	The oral bioavailability of ABT-263 in preclinical animal models is 20% to 50%, depending on formulation. Oral administration of ABT-263 alone induces complete tumor regressions in xenograft models of small-cell lung cancer and acute lymphoblastic leukemia [1]. ABT-263 induced significant prolongation of the EFS distribution in 9 of 35 (26%) of the solid tumor xenografts and in 5 of 6 (83%) of the evaluable ALL xenografts [2]. ABT-263 exhibited a range of antitumor activity, leading to complete tumor regression in several models. Significant regressions of tumors as large as 1 cc were also observed. The efficacy of ABT-263 was also quite durable; in several cases, minimal tumor regrowth was noted several weeks after the cessation of treatment [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
化合物与蛋白结合的复合物	Bcl_2-Navitoclax (ABT-263) Complex
分子量	974.61
分子式	C47H55ClF3N5O6S3
CAS No.	923564-51-6

存储

　|　Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

Ethanol: <1 mg/mL

DMSO: 200 mg/mL (205.21 mM), Need ultrasonic

H2O: <1 mg/mL

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Tse C, et al. ABT-263: a potent and orally bioavailable Bcl-2 family inhibitor. Cancer Res. 2008 May 1;68(9):3421-8. 2. Lock R1, et al. Initial testing (stage 1) of the BH3 mimetic ABT-263 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2008 Jun;50(6):1181-1189. 3. Shoemaker AR, et al. Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clin Cancer Res. 2008 Jun 1;14(11):3268-77. 4. Torres P, Anerillas C, Encinas M, et al. The Motor Neuron Disease Mouse Model hSOD1-G93A Presents a Non-canonical Profile of Senescence Biomarkers in The Spinal Cord[J]. 2020

文献引用

1. Wang S, Wang Z, Wang X, et al. Humanized cerebral organoids-based ischemic stroke model for discovering of potential anti-stroke agents. Acta Pharmacologica Sinica. 2022: 1-11. 2. Torres P, Anerillas C, Ramírez-Núñez O, et al. The motor neuron disease mouse model hSOD1-G93A shows a non-canonical profile of senescence biomarkers. Disease Models & Mechanisms. 2022 3. Torres P, Anerillas C, Ramírez-Núñez O, et al. A motor neuron disease mouse model reveals a non-canonical profile of senescence biomarkers. Disease models & mechanisms. 2022, 15(8): dmm049059. 4. Bhatt H N, Diwan R, Borrego E A, et al.A photothermal driven chemotherapy for the treatment of metastatic melanoma.Journal of Controlled Release.2023, 361: 314-333.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Navitoclax 923564-51-6 Apoptosis BCL inhibit Inhibitor Bcl-2 Family ABT-263 ABT263 ABT 263 inhibitor

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Navitoclax

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