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ABT 199

Cat. No. 6960 1 次引用 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Selective, high affinity Bcl-2 inhibitor; orally bioavailable
别名： Venetoclax,GDC-0199
化学名： 4-[4-[[2-(4-Chlorophenyl)-4,4-dimethyl-1-cyclohexen-1-yl]methyl]-1-piperazinyl]-N-[[3-nitro-4-[[(tetrahydro-2H-pyran-4-yl)methyl]amino]phenyl]sulfonyl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论
文献 (2)
通路 (1)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for ABT 199

ABT 199 is a selective, high affinity Bcl-2 inhibitor (Ki < 0.010 nM). Exhibits >4800-fold selectivity for Bcl-2 over Bcl-xL and Bcl-w, and displays no measurable activity at Mcl-1 (Ki > 444 nM). Potently induces apoptosis in FL5.12-BCL-2 cells (EC50 = 261 nM) and reduces tumor burden in chronic lymphocytic leukemia (CLL) primary samples (EC50 = 3 nM). Shows reduced toxicity to platelets compared to similar compounds. Enhances efficacy of clinically relevant chemotherapy and immunotherapy drugs. Orally bioavailable. Exhibits binding to SARS-CoV-2 3C-like protease (3CLpro) active site in a virtual screen. ABT 199 reverses oxidative phosphorylation in acute myeloid leukemia cells (AML), in vitro and in vivo.

化合物库 for ABT 199

ABT 199 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。

技术数据 for ABT 199

分子量 868.45
公式 C45H50ClN7O7S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1257044-40-8
PubChem ID 49846579
InChI Key LQBVNQSMGBZMKD-UHFFFAOYSA-N
Smiles CC1(C)CCC(CN2CCN(CC2)C2=CC(OC3=CN=C4NC=CC4=C3)=C(C=C2)C(=O)N[S](=O)(=O)C2=CC(=C(NCC3CCOCC3)C=C2)[N](=O)=O)=C(C1)C1=CC=C(Cl)C=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for ABT 199

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 86.84 100

制备储备液 for ABT 199

以下数据基于产品分子量 868.45。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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产品说明书 for ABT 199

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for ABT 199

参考文献是支持产品生物活性的出版物。

Souers et al (2013) ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat.Med. 19 202 PMID: 23291630

Soderquist et al (2018) Systematic mapping of BCL-2 gene dependencies in cancer reveals molecular determinants of BH3 mimetic sensitivity. Nat.Commun. 9 3513 PMID: 30158527

Liu et al (2019) Balancing apoptosis and autophagy for Parkinson's disease therapy: targeting BCL-2. ACS Chem.Neurosci. 10 792 PMID: 30400738

Bosc et al (2021) Mitochondrial inhibitors circumvent adaptive resistance to venetoclax and cytarabine combination therapy in acute myeloid leukemia. Nat.cancer 2 1204 PMID: 35122057

If you know of a relevant reference for ABT 199, please let us know.

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关键词: ABT 199, ABT 199 supplier, ABT199, GDC, 0199, GDC0199, Bcl-2, inhibitors, inhibits, induces, apoptosis, orally, bioavailable, selective, high, affinity, SARS-CoV-2, 3C-like, protease, severe, acute, respiratory, syndrome, coronavirus, COVID-19, Venetoclax, GDC-0199, Family, 3C, and, 3CL, Proteases, 6960, Tocris Bioscience

1 篇 ABT 199 的引用文献

引用文献是使用了 Tocris 产品的出版物。 ABT 199 的部分引用包括：

Håkon et al (2020) Targeting Cellular Metabolism in Acute Myeloid Leukemia and The Role of Patient Heterogeneity. Cells 9 PMID: 32392896

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该领域的文献

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