COTI-2

CAS: 1039455-84-9 货号: C420437 分子式: C19H22N6S 分子量: 366.48
有货
级别和纯度: 10mM in DMSO
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
C420437-1ml
现货 Stock Image
¥302.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


Information

COTI-2 COTI-2 is an orally available third generation thiosemicarbazone and activator of mutant forms of the p53 protein, with potential antineoplastic activity.

Targets

p53 mutants

In vitro

The thiosemicarbazone COTI-2 is reported to promote refolding of mutant p53 and restore wild-type-p53 function. It is active against human tumour cell lines of various origins at nanomolar concentrations, induces cell death by apoptosis. COTI-2 is highly efficacious against multiple cancer cell lines from a broad range of human cancers both in vitro and in vivo. COTI-2 does not significantly inhibit over 200 kinases from major kinase pathways involved in cancer that were evaluated in both kinase assays and does not inhibit the ATPase activity of Hsp90, a ubiquitous molecular chaperone that plays an essential role in cell survival and cell cycle control.

In vivo

COTI-2 significantly inhibited tumor growth in the HT-29 human colorectal tumor xenografts at a dose of 10 mg/kg. COTI-2 also significantly inhibited tumor growth in the SHP-77 SCLC xenograft model at a dose as low as 3 mg/kg. Its treatment delays U87-MG, MDA-MB-231 and OVCAR-3 xenograft growth. COTI-2 treatment demonstrates a safe toxicity profile in vivo. COTI-2 selectively targets a wide variety of human cancer cell lines, as demonstrated by the in vitro data, while having little deleterious effects on normal cells.

Cell Research(from reference)

Cell lines:SHP-77 cells 

Concentrations:100, 250, 1000 nM 

Incubation Time:48 h 

规格

英文别名
1-​Piperazinecarbothioi​c acid,4-​(2-​pyridinyl)​-​,2-​(6,​7-​dihydro-​8(5H)​-​quinolinylidene)​hydrazide
规格或纯度
10mM in DMSO
英文名称
COTI-2
生化机理
COTI-2 是一种可口服的第三代硫代氨基羰基化合物,是 p53 蛋白突变形式的激活剂,具有潜在的抗肿瘤活性。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
PubChem SID
分子类型
小分子
IUPAC Name
N-(6,7-dihydro-5H-quinolin-8-ylideneamino)-4-pyridin-2-ylpiperazine-1-carbothioamide
INCHI
1S/C19H22N6S/c26-19(23-22-16-7-3-5-15-6-4-10-21-18(15)16)25-13-11-24(12-14-25)17-8-1-2-9-20-17/h1-2,4,6,8-10H,3,5,7,11-14H2,(H,23,26)
InChi Key
UTDAKQMBNSHJJB-UHFFFAOYSA-N
Smiles
C1CC2=C(C(=NNC(=S)N3CCN(CC3)C4=CC=CC=N4)C1)N=CC=C2
Isomeric SMILES
C1CC2=C(C(=NNC(=S)N3CCN(CC3)C4=CC=CC=N4)C1)N=CC=C2
分子量
366.48
Reaxy-Rn
18407829
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18407829&ln=

技术文档

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高级数据

三维结构
交互式化学结构模型





产品属性
ALogP 3.825
hba_count 3
HBD Count 1
Rotatable Bond 4
化学和物理性质
DMSO(mg / mL) Max Solubility
73
DMSO(mM) Max Solubility
199.1923161
Water(mg / mL) Max Solubility
<1
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批号(Lot Number) 证书类型 货号
I2419158 分析证书 C420437
溶液计算器