C188-9 - Moligand™, 10mM in DMSO , Inhibitor of signal transducer and activator of transcription 3, CAS No.432001-19-9, Inhibitor of signal transducer and activator of transcription 3

CAS: 432001-19-9 Cat. No.: C408822 분자식: C₂₇H₂₁NO₅S 분자량: 471.52 EC 번호: 836-653-0

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

TTI 101 | Benzenesulfonamide, N-​(1',​2-​dihydroxy[1,​2'-​binaphthalen]​-​4'-​yl)​-​4-​methoxy-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

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%

Specifications

동의어

TTI 101 | Benzenesulfonamide, N-​(1',​2-​dihydroxy[1,​2'-​binaphthalen]​-​4'-​yl)​-​4-​methoxy-

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

C188-9 (TTI 101) is a potent inhibitor of STAT3 that 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.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

INHIBITOR

작동 메커니즘

Inhibitor of signal transducer and activator of transcription 3

제품 특성

• ALogP: 5.152
• hba_count: 3
• HBD 수: 3
• 회전 가능한 결합: 5

이름과 식별자

• 이성체 SMILES: COC1=CC=C(C=C1)S(=O)(=O)NC2=CC(=C(C3=CC=CC=C32)O)C4=C(C=CC5=CC=CC=C54)O
• 대체 CAS: 432001-19-9
• MeSH 용어: C188-9 compound;N-(4-hydroxy-3-(2-hydroxynaphthalen-1-yl)naphthalen-1-yl)-4-methoxybenzenesulfonamide;STAT3 inhibitor TTI-101;TTI-101
• 분자량: 471.52
• Reaxy-Rn: 23997464
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23997464&ln=

관련 대상(인간)

STAT3 Tchem Signal transducer and activator of transcription 3 (0 Activities)

Discover Target: STAT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

화학 및 물리적 특성

• 용해성: Solubility (25°C) In vitro DMSO: 62 mg/mL (199.69 mM); Ethanol: 62 mg/mL (199.69 mM); Water: Insoluble
• DMSO(mg/mL) 최대 용해도: 94
• DMSO(mM) 최대 용해도: 199.3552766
• 물(mg/mL) 최대 용해도: ＜1