计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
概述
产品介绍：
Navitoclax (ABT-263)是一种有效的Bcl-xL，Bcl-2和Bcl-w抑制剂，无细胞试验中Ki分别为≤0.5 nM，≤1 nM和≤1 nM，但与Mcl-1和A1结合微弱。
Navitoclax (ABT-263) 是有效的 Bcl-2 抑制剂，可与Bcl-xL，Bcl-2， Bcl-w等多种Bcl-2家族蛋白结合，Ki 值小于 1 nM。
Information
Navitoclax (ABT-263) is a potent inhibitor ofBcl-xL,Bcl-2andBcl-wwithKiof ≤ 0.5 nM, ≤1 nM and ≤1 nM in cell-free assays, but binds more weakly to Mcl-1 and A1. Phase 2.
In vitro
ABT-263 is structurally related to ABT-737; it is a disruptor of Bcl-2/Bcl-xL interactions with pro-apoptotic proteins. Overexpression of the prosurvival Bcl-2 family members is commonly associated with tumor maintenance, progression, and chemoresistance. ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. A wide range of cellular activity is observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nM against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) results in an EC50 at 22 μM. All four cell lines with EC50 values of <400 nM (H146, H889, H1963, and H1417) are also highly sensitive to ABT-737, and the two most resistant lines (H1048 and H82) are similarly resistant to ABT-263.
In vivo
When ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume. Oral administration of ABT-263 alone causes complete tumor regressions in xenograft models of small-cell lung cancer and acute lymphoblastic leukemia. In xenograft models of aggressive B-cell lymphoma and multiple myeloma where ABT-263 displays modest or no single agent activity, it significantly enhances the efficacy of clinically relevant therapeutic regimens.
Cell Data
cell lines：
Concentrations：0-1 μM
Incubation Time：48 hours
Powder Purity:≥98%
规格
别名
纳维托克拉(ABT-263)
规格或纯度
10mM in DMSO
英文名称
Navitoclax (ABT-263)
生化机理
Navitoclax（ABT-263）是Bcl-xL、Bcl-2和Bcl-w的强效抑制剂，在无细胞实验中的Ki分别为≤0.5 nM、≤1 nM和≤1 nM，但与Mcl-1和A1的结合力较弱。第 2 阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1(CCC(=C(C1)CN2CCN(CC2)C3=CC=C(C=C3)C(=O)NS(=O)(=O)C4=CC(=C(C=C4)N[C@H](CCN5CCOCC5)CSC6=CC=CC=C6)S(=O)(=O)C(F)(F)F)C7=CC=C(C=C7)Cl)C
分子量
974.61
Reaxy-Rn
15630714
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=15630714&ln=
高级数据
产品属性
| ALogP | 9.6 |
|---|
关联靶点（人）
MCL1
Tchem
诱导髓系白血病细胞分化蛋白Mcl-1(Induced myeloid leukemia cell differentiation protein Mcl-1)
(2 活性数据)
BCL2
Tclin
凋亡调节剂Bcl-2(Apoptosis regulator Bcl-2)
(5 活性数据)
BCL2L1
Tchem
Bcl-2类蛋白1(Bcl-2-like protein 1)
(6 活性数据)
BCL2L2
Tchem
Bcl-2类蛋白2(Bcl-2-like protein 2)
(2 活性数据)
ASPH
Tchem
天冬氨酰/天冬酰胺酰β-羟化酶(Aspartyl/asparaginyl beta-hydroxylase)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 64 mg/mL (197.3 mM); Water: Insoluble; Ethanol: Insoluble;
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
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危险品化学品经营许可证（带存储）