CB-5083 - 10mM in DMSO , CAS No.1542705-92-9

CAS: 1542705-92-9 Cat. No.: C408056 분자식: C₂₄H₂₃N₅O₂ 분자량: 413.47

등급 & 순도 10mM in DMSO

Synonyms

1H-​Indole-​4-​carboxamide, 1-​[7,​8-​dihydro-​4-​[(phenylmethyl)​amino]​-​5H-​pyrano[4,​3-​d]​pyrimidin-​2-​yl]​-​2-​methyl-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

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%

사양

동의어

1H-​Indole-​4-​carboxamide, 1-​[7,​8-​dihydro-​4-​[(phenylmethyl)​amino]​-​5H-​pyrano[4,​3-​d]​pyrimidin-​2-​yl]​-​2-​methyl-

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

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

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

INHIBITOR

제품 특성

ALogP

3.748

hba_count

4

HBD 수

2

회전 가능한 결합

5

이름과 식별자

이성체 SMILES

CC1=CC2=C(C=CC=C2N1C3=NC4=C(COCC4)C(=N3)NCC5=CC=CC=C5)C(=O)N

분자량

413.47

Reaxy-Rn

26539278

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26539278&ln=

관련 대상(인간)

VCP Tchem Transitional endoplasmic reticulum ATPase (6 Activities)

Discover Target: VCP

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

화학 및 물리적 특성

• DMSO(mg/mL) 최대 용해도: 82
• DMSO(mM) 최대 용해도: 198.3215227
• 물(mg/mL) 최대 용해도: ＜1