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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > Apoptosis > VenetoclaxCAS：1257044-40-8
Molecular Formula：C45H50ClN7O7S
Molecular Weight：868.44
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥97%
Appearance：Light yellow to yellow Solid
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| CAS | 1257044-40-8 |
| Name | Venetoclax |
| Molecular Formula | C45H50ClN7O7S |
| Molecular Weight | 868.44 |
| Solubility | Soluble in DMSO |
| Purity | ≥97% |
| Appearance | Light yellow to yellow Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 820-130-9 |
| MDL | MFCD23160052 |
| SMILES | O=C(NS(=O)(C1=CC=C(NCC2CCOCC2)C([N+]([O-])=O)=C1)=O)C3=CC=C(N4CCN(CC5=C(C6=CC=C(Cl)C=C6)CC(C)(C)CC5)CC4)C=C3OC7=CN=C(NC=C8)C8=C7 |
| Target Point | Bcl-2 |
| Passage | Apoptosis |
| Background | Venetoclax is a potent and selective Bcl-2 inhibitor. |
| Biological Activity | Venetoclax (GDC-0199; ABT-199) 是一种高效，有选择性和口服活性的 Bcl-2 抑制剂，Ki 小于0.01 nM。[1-3] |
| In Vitro | Venetoclax(ABT-199)有效杀死FL5.12-BCL-2细胞(EC50 = 4nM)，Venetoclax(ABT-199)对FL5.12-BCL-XL细胞显示出更弱的活性(EC50 = 261nM)。 ABT-199还显示细胞哺乳动物双杂交分析中的选择性，其中它破坏BCL-2-BIM复合物(EC50 = 3 nM)，但对BCL-XL-BCL-XS(EC50 =2.2μM)或MCL的效果要差得多[1]。 |
| In Vivo | 在来自RS4; 11细胞(ALL)的异种移植物中单次口服12.5mg / kg体重后，Venetoclax(ABT-199)引起最大肿瘤生长抑制(TGImax)为47％(P <0.001)和肿瘤生长延迟(TGD)为26％(P <0.05)[1]。用Venetoclax(ABT-199)100mg / kg处理建立的异种移植(T-ALL细胞系LOUCY的小鼠异种移植模型)肿瘤4天导致白血病负荷显着减少(P = 0.0048)[2]。 |
| Cell Experiment | 将RS4; 11个细胞以每孔50，000个接种于96孔板中，并用在1μM开始并以0.00005μM结束的半对数步骤稀释的化合物处理。将所有其他白血病和淋巴瘤细胞系以每孔15，000-20，000个细胞接种在适当的培养基中，并与Venetoclax或Navitoclax孵育48小时。使用Cell TiterGlo试剂测定对增殖的影响。 EC50值通过浓度 - 响应数据的非线性回归分析确定。繁殖并评估小鼠FL5.12-BCL-2和FL5.12-BCL-XL细胞。将Bak - / - Bax - / - 双敲除小鼠胚胎成纤维细胞以每孔5，000个细胞接种到96孔微量滴定板中，在补充有10％FBS的DMEM中。将相同培养基中的Venetoclax(ABT-199)以5μM开始以半对数稀释度添加。然后将细胞在37℃(5％CO 2)下孵育48小时，并使用Cell TiterGlo试剂[1]测定对增殖的影响。 |
| Animal Experiment | 小鼠[2]非肥胖糖尿病/重症联合免疫缺陷γ(NSG)小鼠在尾静脉6周龄时注射含有5×106荧光素酶标记的LOUCY细胞的150μL磷酸盐缓冲盐水。在常规时间点，使用IVIS Lumina II成像系统测量生物发光。在第6周时，移植细胞并将小鼠随机分成2组(两组中男性和女性的数量相等)，并在第0天开始治疗。小鼠用Venetoclax治疗(ABT-199)100mg/kg体重或通过口服强饲法连续4天。在第0天，第2天和第4天，测量生物发光。在成像之前，给小鼠腹膜内注射200μL的15mg/mL萤火虫D-荧光素钾盐溶液，并通过吸入5％异氟烷麻醉。在注射荧光素后10分钟对小鼠成像。通过Living Image软件中的感兴趣区域工具(总计数)计算每只小鼠中的总生物发光信号。 |
| Data Literature Source | [1]. Souers AJ，et al. ABT-199，a potent and selective BCL-2 inhibitor，achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8. [2]. Peirs S，et al. ABT-199 mediated inhibition of BCL-2 as a novel therapeutic strategy in T-cell acute lymphoblastic leukemia. Blood. 2014 Dec 11;124(25):3738-47. [3]. Bi C，et al. Inhibition of 4EBP phosphorylation mediates the cytotoxic effect of mechanistic target of rapamycin kinase inhibitors in aggressive B-cell lymphomas. Haematologica. 2017 Apr;102(4):755-764. |
| Unit | Bottle |
| Specification | 2mg 5mg 10mg |
Venetoclax是一种高效，有选择性的 Bcl-2 抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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