ABT-263

目录号 M1637 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

ABT-263 (Navitoclax)是一种有效的Bcl-xL， Bcl-2和Bcl-w抑制剂，K_i分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。

别名：Navitoclax

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
10mM*1mL in DMSO	¥ 900	中国库存现货
5mg	¥ 500	中国库存现货
10mg	¥ 850	中国库存现货
50mg	¥ 2200	中国库存现货
100mg	¥ 3200	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 99.79%
COA
MSDS
H-NMR
HPLC

产品信息

生物活性

ABT-263 (Navitoclax)是一种有效的Bcl-xL， Bcl-2和Bcl-w抑制剂，K_i分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。ABT-263有效抑制Bcl-2蛋白家族，用荧光偏振分析法测试ABT-263作用于Bcl-xL, Bcl-2和 Bcl-w时，K_i分别为0.5, 1和1 nM。ABT-263结构上与ABT-737相关。ABT-263阻断Bcl-2 和Bcl-XL与凋亡前体蛋白相互作用。

使用AbMole产品发表的文献

Cancers (Basel). 2021 Jan 19;13(2):361.

Identification of a Dexamethasone Mediated Radioprotection Mechanism Reveals New Therapeutic Vulnerabilities in Glioblastoma
Cancer Res. 2020 Apr 1;80(7):1387-1400.

Inhibition of BCL2 Family Members Increases the Efficacy of Copper Chelation in BRAF V600E-Driven Melanoma.
Clin Cancer Res. 2019 Jan 1;25(1):312-324.

NOTCH1 Represses MCL-1 Levels in GSI-resistant T-ALL, Making them Susceptible to ABT-263
Cell Death and Disease. 2018 Jan 26;9:137-52.

Downregulation of MCL-1 and upregulation of PUMA using mTOR inhibitors enhance antitumor efficacy of BH3 mimetics in triple-negative breast cancer
Clin Cancer Res. 2017 Oct 19;pii: clincanres.1577.2017.

Epithelial-to-mesenchymal transition antagonizes response to targeted therapies in lung cancer by suppressing BIM
Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):E1288-96.

Assessment of ABT-263 activity across a cancer cell line collection leads to a potent combination therapy for small-cell lung cancer.

产品使用成果展示

	数据来源	Cell Death & Disease (2018). Figure 6. ABT263 (Abmole Bioscience)
	方法	IHC analysis
	细胞系/动物模型	Tumor-bearing nude mice
	浓度	25 mg/kg
	处理时间	4 weeks
	实验结果	Following BEZ235 treatment with or without ABT263, the expression of MCL-1 was suppressed while PUMA was increased; correspondingly, the expressions of p-AKT and p-4EBP1 were significantly suppressed.

	数据来源	Cell Death & Disease (2018). Figure 5. ABT263 (Abmole Bioscience)
	方法	i.p.
	细胞系/动物模型	Tumor-bearing nude mice
	浓度	25 mg/kg
	处理时间	4 weeks
	实验结果	Our results showed that combination therapy of BEZ235 and ABT263 significantly suppressed tumor growth, comparing with each drug treatment alone.

	数据来源	Cell Death & Disease (2018). Figure 4. ABT263 (Abmole Bioscience)
	方法	CO-IP analysis
	细胞系/动物模型	MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells
	浓度	1 μM
	处理时间	24 h
	实验结果	Additionally, the interaction between MCL-1 and BAK was also significantly increased following mono treatment of ABT263.

	数据来源	Cell Death & Disease (2018). Figure 3. ABT263 (Abmole Bioscience)
	方法	Immunoblotting analysis
	细胞系/动物模型	MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells
	浓度	1 μM
	处理时间	24 h
	实验结果	Of note, we found that, besides MCL-1, the expression of PUMA but not other members was significantly increased following treatment of BEZ235 with or without ABT263 in MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells.

	数据来源	Cell Death & Disease (2018). Figure 2. ABT263 (Abmole Bioscience)
	方法	Cell viability analysis
	细胞系/动物模型	MDA-MB-231, MDA-MB-157, and MDA-MB-468 cells
	浓度	1 μM
	处理时间	24 h
	实验结果	The cell viability following indicated treatments was observed and the result showed that mTORC1/2 inhibitors (BEZ235 or AZD8055) incombination with ABT263 significantly inhibited cell viability in MDA-MB-231, MDA-MB-157, and MDAMB- 468 cells, comparing with each compound treatment alone.

	数据来源	Clin Cancer Res (2017). Figure 4. ABT-263 (Abmole Bioscience)
	方法	vitro observations
	细胞系/动物模型	Mice harboring H1975 ER-TWIST+4-OHT tumors
	浓度	80mg/kg
	处理时间	5 d
	实验结果	The pharmaceutical approach of combining ABT-263 and an EGFRi could be successful in both EGFR mutant lung cancers with EMT-mediated acquired resistance, as well as mesenchymal cancers in the upfront setting.

	数据来源	Proc Natl Acad Sci U S A. (2015). Figure 3. ABT-263 and AZD8055 were purchased from Active Biochemicals (Hong Kong, China) and Abmole Bioscience (Houston, TX)
	方法	FACS analysis(Apoptosis), Western blotting, Immunoprecipitation (IP),Traditional human cell-line xenograft experiments
	细胞系/动物模型	SCLC H82 and H1048 cells
	浓度	500 nM AZD8055, 1 μM ABT-263
	处理时间	2,16, 72h
	实验结果	Combination treatment with ABT-263 and the TORC1/2 inhibitor AZD8055 leads to robust apoptosis and antitumor activity in vivo.

	数据来源	Proc Natl Acad Sci U S A. (2015). Figure 2. ABT-263 and AZD8055 were purchased from Active Biochemicals (Hong Kong, China) and Abmole Bioscience (Houston, TX)
	方法	FACS analysis(Apoptosis),quantitative (q)RT-PCR, Western blotting, Immunoprecipitation (IP)
	细胞系/动物模型	SCLC SW1271 and H1048 cells
	浓度	1µM
	处理时间	6,48,72h
	实验结果	BIM and MCL-1 mediate ABT-263–induced apoptosis in SCLC, and the ratio of BIM to MCL-1 expression predicts the magnitude of apoptosis in SCLC cell lines.

	数据来源	Proc Natl Acad Sci U S A. (2015). Figure 1. ABT-263 and AZD8055 were purchased from Active Biochemicals (Hong Kong, China) and Abmole Bioscience (Houston, TX)
	方法	quantitative (q)RT-PCR
	细胞系/动物模型	SCLC cell lines
	浓度	1µM
	处理时间	72h
	实验结果	we found a modest, but significant, correlation between BIM expression and sensitivity to ABT-263.ABT-263 across both data sets (SI Appendix, Fig. S1 B and C). However, the ratio of BIM to MCL-1 predicted sensitivity to ABT-263 more effectively than the expression of either biomarker alone. SCLC lines have increased BIM expression compared with other solid tumor types along with enhanced sensitivity to ABT-263 compared with other solid tumor types across a large panel of cancer cell lines.

实验参考

体外实验*
细胞系	H1048 cells
方法	Flourescence Activated Cell Sorting (FACS) for death assays and cell cycle analysis Cells were plated in triplicate in 6-well plates or 6-cm dishes to reach ~30-40% confluency the next day. On the next day, cells were treated with the indicated drugs or no drug control. Apoptosis and cell cycle experiments were performed essentially as previously described and analyzed on a BD LSR III (Becton Dickenson, Franklin Lanes, NJ). The cell cycle experiments were gated to include only viable cells in order for the cell cycle distribution to be determined from this population. For apoptosis assays, the number of cells in quadrants II and IV (Annexin positive) were counted as apoptotic, where cells with subG0/G1 DNA3 were quantified and counted as apoptotic following staining with PI. The Annexin stain was conjugated to FITC and the analysis was done on a Guava easyCyte flow cytometer (EMD Millipore (Temecula, CA)). In the engineered H1048 cells, apoptosis determined by ABT-263 treatment and combination ABT-263/AZD8055 treatment were performed within the same experiment.
浓度	500 nM AZD8055, 1 μM ABT-2631
处理时间	72h

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
动物模型	Traditional human cell-line xenograft(6-10 week-old mice with a Nu/Nu background with exponentially growing NCI-H1048 or NCI-H82 cells into the right rear flanks)
配制	AZD8055 was dissolved in Captisol ®. ABT-263 was dissolved in a mixture of 60% Phosal 50 PG, 30% PEG 400 and 10% EtOH.
剂量	16 mg/kg/qd AZD8055, 80 mg/kg/qd ABT-263
给药处理	oral gavage

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	974.61
分子式	C47H55ClF3N5O6S3
CAS号	923564-51-6
溶解性（25°C）	DMSO ≥100 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.0261 mL	5.1303 mL	10.2605 mL
5 mM	0.2052 mL	1.0261 mL	2.0521 mL
10 mM	0.1026 mL	0.513 mL	1.0261 mL

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	小鼠	大鼠	兔	豚鼠	仓鼠	狗
重量 (kg)	0.02	0.15	1.8	0.4	0.08	10
体表面积 (m²)	0.007	0.025	0.15	0.05	0.02	0.5
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m系数

例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Faber AC,et.al. Proc Natl Acad Sci U S A. Assessment of ABT-263 activity across a cancer cell line collection leads to a potent combination therapy for small-cell lung cancer.

[2] Yamaguchi et al. PLoS One. Efficient elimination of cancer cells by deoxyglucose-ABT-263/737 combination therapy.

[3] Shi et al. Cancer Res. Navitoclax (ABT-263) accelerates apoptosis during drug-induced mitotic arrest by antagonizing Bcl-xL.

[4] Gandhi et al. J Clin Oncol. Phase I study of Navitoclax (ABT-263), a novel Bcl-2 family inhibitor, in patients with small-cell lung cancer and other solid tumors.

[5] Tahir et al. Mol Cancer Ther. Identification of expression signatures predictive of sensitivity to the Bcl-2 family member inhibitor ABT-263 in small cell lung carcinoma and leukemia/lymphoma cell lines.

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