A-1331852
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.
作用于BCL-2TR-FRET,Ki为6 nM。
A-1331852是一种强效的和选择性的BCL-XL抑制剂。
据报道,凋亡由密切相关的蛋白家族调节,例如首个发现的家族成员B细胞淋巴瘤蛋白2(BCL-2)。 BCL-2家族蛋白分为一至四个BCL-2同源基序,并且可以进一步细分为促细胞凋亡和抗细胞凋亡亚群。
体外:A-1331852被鉴定为一种强效的BCL-XL抑制剂,细胞活性比其类似物A-1155463和先前报道的BCL-XL抑制剂navitoclax分别强10至50倍。此外,在BCL-XL依赖性Molt-4细胞中,A-1331852可以选择性地破坏BCL-XL-BIM复合物并诱导凋亡标志物,中值IC50在低纳摩尔范围内,但不影响无BAK或BAX的MEF细胞[1]。
体内:先前的动物研究发现,A-1331852作为单一药剂在Molt-4异种移植模型中可以表现出抗肿瘤功效,例如肿瘤消退。此外,在SCLC的NCI-H1963.FP5异种移植模型中,研究发现A-1331852与venetoclax联合用药能够重现navitoclax的功效[1]。
临床试验:到目前为止,A-1331852仍处于临床前研究阶段。
参考文献:
[1] Leverson JD et al. Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci Transl Med.2015 Mar 18;7(279):279ra40. doi: 10.1126/scitranslmed.aaa4642.
- 1. Anna L. Koessinger, Catherine Cloix, et al. "Increased apoptotic sensitivity of glioblastoma enables therapeutic targeting by BH3-mimetics." Cell Death Differ. 2022 Apr 26. PMID: 35473984
- 2. Shahbandi A, Rao SG, et al. "BH3 mimetics selectively eliminate chemotherapy-induced senescent cells and improve response in TP53 wild-type breast cancer." Cell Death Differ. 2020;10.1038/s41418-020-0564-6. PMID: 32457483
Storage | Store at -20°C |
M.Wt | 658.81 |
Cas No. | 1430844-80-6 |
Formula | C38H38N6O3S |
Solubility | ≥113.6 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 3-(1-(adamantan-1-ylmethyl)-5-methyl-1H-pyrazol-4-yl)-6-(8-(benzo[d]thiazol-2-ylcarbamoyl)-3,4-dihydroisoquinolin-2(1H)-yl)picolinic acid |
SDF | Download SDF |
Canonical SMILES | O=C(C1=NC(N2CC3=C(C=CC=C3C(NC4=NC5=CC=CC=C5S4)=O)CC2)=CC=C1C6=C(C)N(CC78CC9CC(C8)CC(C9)C7)N=C6)O |
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。 |
质量控制和MSDS
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