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

CAS: 1542705-92-9 Cat. No.: C408056 分子式: C₂₄H₂₃N₅O₂ 分子量: 413.47

グレード＆純度 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

概要

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%

仕様

同義語

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

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

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

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

アクションタイプ

INHIBITOR

製品の性質

ALogP

3.748

hba_count

4

HBD数

2

回転可能な結合

5

名前と識別子

異性体SMILES

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

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=

関連ターゲット（人間）

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)

化学的性質と物理的性質

• DMSO（mg / mL） 最大溶解度: 82
• DMSO（mM） 最大溶解度: 198.3215227
• 水（mg / mL） 最大溶解度: ＜1