CB-5083

p97 Inhibitors
  • 10mM in DMSO
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
C408056-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 1H-​Indole-​4-​carboxamide, 1-​[7,​8-​dihydro-​4-​[(phenylmethyl)​amino]​-​5H-​pyrano[4,​3-​d]​pyrimidin-​2-​yl]​-​2-​methyl-
规格或纯度 10mM in DMSO
英文名称 CB-5083
生化机理 CB-5083 是一种强效、选择性、可口服的 p97 AAA ATPase 抑制剂,IC50 为 11 nM。第一阶段
储存温度 -80℃储存
运输条件 超低温冰袋运输
产品介绍

CB-5083是一种有效的,选择性的,且口服具有生物活性的p97 AAA ATPase抑制剂,IC50为 11 nM。Phase 1。

Information

CB-5083 CB-5083 is a potent, selective, and orally bioavailable p97 AAA ATPase inhibitor with IC50 of 11 nM. Phase 1.
In vitro

In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM.

In vivo

In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition.
Cell Data

cell lines:

Concentrations:~40.0 μM

Incubation Time:72 h

Powder Purity:≥98%

产品属性

ALogP 3.748
hba_count 4
HBD Count 2
Rotatable Bond 5

关联靶点(人)

VCP Tchem 过渡内质网ATP酶(Transitional endoplasmic reticulum ATPase) (6 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CC1=CC2=C(C=CC=C2C(N)=O)[N]1C3=NC4=C(COCC4)C(=N3)NCC5=CC=CC=C5
分子量 413.47
Reaxy-Rn 26539278
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26539278&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 82
DMSO(mM) Max Solubility 198.32
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 26539278
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26539278&ln=

技术规格说明书

Record the entire process by video Conform
Concentration(Compounding value) 9-11(mmol/L)

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:

溶液计算器

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