ABT-199
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ABT-199是通过基于结构的逆向过程而研发的,是一种新型的特异性BCL-2抑制剂,具有低浓度的亲和力。ABT-199通过抑制细胞凋亡的线粒体途径,从而杀死非霍奇金淋巴瘤(NHL)和急性骨髓性白血病细胞系,以及BCL-2依赖而非BCL-XL依赖性的细胞,展示了对一系列血液系统肿瘤的抗肿瘤活性,同时保留了血小板。据报道,在几种人类血液系统肿瘤的异种移植模型中,ABT-199能够抑制肿瘤的生长。
参考文献:
Matthew S. Davids and Anthony Letai. ABT-199: a new hope for selective BCL-2 inhibition. Cancer Cell 2013; 23(2): 139-141
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 868.44 |
Cas No. | 1257044-40-8 |
Formula | C45H50ClN7O7S |
Synonyms | ABT199, ABT 199, GDC0199, GDC-0199 |
Solubility | ≥43.42 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide |
SDF | Download SDF |
Canonical SMILES | CC1(CCC(=C(C1)C2=CC=C(C=C2)Cl)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)NS(=O)(=O)C5=CC(=C(C=C5)NCC6CCOCC6)[N+](=O)[O-])OC7=CN=C8C(=C7)C=CN8)C |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
正常人B细胞,CD4+和CD8+ T细胞 |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
24 h;4 μM |
应用 |
评估健康人外周血样品中的正常人B细胞,CD4+和CD8+ T细胞对ABT-199的敏感性,正常外周B细胞比T细胞亚群的敏感性高1000倍作用(B细胞、CD4 T细胞和CD8 T细胞的平均LC50值分别为3.0±0.9 nM、2.5±0.6 μM 和1.3±0.7 μM,B细胞与CD4 T细胞:P=0.008;B细胞与CD8 T细胞:P=0.004)。这些结果表明,不像T细胞和骨髓细胞,正常人外周血B细胞对ABT-199是高度敏感的。 |
动物实验[1]: | |
动物模型 |
Eu-Myc小鼠 |
剂量 |
100 mg/kg;口服给药 |
应用 |
评估ABT-199(100 mg/kg)短期治疗对淋巴细胞亚群的体内效果,ABT-199口服给药后减少外周B细胞,与其在体外对小鼠和人细胞的效果类似。这些数据表明,由于对关键B/T前体细胞中选择性Bcl-2抑制的内在不敏感性,ABT-199的长期使用在较小程度上可能会影响正常淋巴细胞。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Khaw S L, Mérino D, Anderson M A, et al. Both leukaemic and normal peripheral B lymphoid cells are highly sensitive to the selective pharmacological inhibition of prosurvival Bcl-2 with ABT-199[J]. Leukemia, 2014, 28(6): 1207-1215. |
ABT-199 (GDC-0199)是一种选择性的Bcl-2抑制剂,Ki值<0.01 nM, 比对Bcl-xL和Bcl-w的选择性高4800倍。 | ||||||
靶点 | Bcl-2 | |||||
IC50 | < 0.010 nM (Ki) |
质量控制和MSDS
- 批次: