C188-9, 信号转导和转录激活因子 3 抑制剂

STAT3 Selective Inhibitors | Activators

Moligand™

10mM in DMSO

CAS编号: 432001-19-9(DMSO)
分子式: C₂₇H₂₁NO₅S
分子量: 471.52

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
C408822-1ml	1ml	现货

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Compound libraries (12332)

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基本描述

英文别名	TTI 101 \| Benzenesulfonamide, N-(1',2-dihydroxy[1,2'-binaphthalen]-4'-yl)-4-methoxy-
规格或纯度	Moligand™, 10mM in DMSO
英文名称	C188-9
生化机理	C188-9（TTI 101）是一种强效的 STAT3 抑制剂，能以高亲和力（KD=4.7±0.4 nM）与 STAT3 结合。C188-9 在小鼠体内的耐受性良好，口服生物利用度高，并能在肿瘤中富集。
储存温度	-80℃储存
运输条件	超低温冰袋运输
作用类型	抑制剂
作用机制	信号转导和转录激活因子 3 抑制剂
产品介绍	C188-9 (TTI-101) 是 Stat3 的抑制剂，其 Kd 值为 4.7 nM。C188-9 抑制 G-CSF 诱导的 STAT3 激活和 STAT3 依赖性基因表达。C188-9 诱导 AML 细胞系和原代标本凋亡，抑制原代 AML 细胞集落形成。 Information C188-9 (TTI 101) is a potent inhibitor ofSTAT3that binds to STAT3 with high affinity (KD=4.7±0.4 nM). C188-9 is well tolerated in mice, shows good oral bioavailability, and is concentrated in tumors. In vitro C188-9 is a small-molecule inhibitor of Stat3 that targets the phosphotyrosyl peptide binding site within the Stat3 Src homology 2 (SH2) domain with Ki 136 nM. It does not inhibit upstream Jak or Src kinases. In vivo Treatment of nude mice bearing xenografts of UM-SCC-17B, a radioresistant HNSCC line, with C188-9, but not C188, prevented tumor xenograft growth. C188-9 was well tolerated in mice, showed good oral bioavailability, and was concentrated in tumors. Cell Data cell lines：CD34⁺ cells Concentrations：0, 0.1, 0.3, 1, 3, 10, 30 μM Incubation Time：24 h Powder Purity:≥98%

产品属性

ALogP	5.152
hba_count	3
HBD Count	3
Rotatable Bond	5

关联靶点（人）

STAT3 Tchem 信号转导和转录激活因子 3(Signal transducer and activator of transcription 3) (0 活性数据)

点击查看靶蛋白信息： STAT3

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

Canonical SMILES	COC1=CC=C(C=C1)[S](=O)(=O)NC2=CC(=C(O)C3=CC=CC=C23)C4=C(O)C=CC5=C4C=CC=C5
分子量	471.52
Reaxy-Rn	23997464
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23997464&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 62 mg/mL (199.69 mM); Ethanol: 62 mg/mL (199.69 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility	94
DMSO(mM) Max Solubility	199.36
Water(mg / mL) Max Solubility	<1