CB-5083 1-(4-(苄基氨基)-7,8-二氢-5H-吡喃并[4,3-d]嘧啶-2-基)-2-甲基-1H-吲哚-4-甲酰胺

CAS 1542705-92-9 MFCD642705929

化学结构图

1542705-92-9
SMILES: Cc1cc2c(C(N)=O)cccc2n1-c1nc2c(c(NCc3ccccc3)n1)COCC2

化学属性

Mol. Weight413.4

别名和识别编码

PubChem Substance ID73051434
InChIInChI=1S/C24H23N5O2/c1-15-12-18-17(22(25)30)8-5-9-21(18)29(15)24-27-20-10-11-31-14-19(20)23(28-24)26-13-16-6-3-2-4-7-16/h2-9,12H,10-11,13-14H2,1H3,(H2,25,30)(H,26,27,28)
Synonym (1-(4-(benzylamino)-5H,7H,8H-pyrano(4,3-d)pyrimidin-2-yl))-2-methyl-1H-indole-4-carboxamide CB-5083 CB5083; CB-5083; CB 5083.
Chemical NameCB-5083
Chemical Name Translation1-(4-(苄基氨基)-7,8-二氢-5H-吡喃并[4,3-d]嘧啶-2-基)-2-甲基-1H-吲哚-4-甲酰胺
FormulaC24H23N5O2
IUPAC Name1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide
InChIKeyRDALZZCKQFLGJP-UHFFFAOYSA-N
Canonical SMILESO=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N.
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产品应用

  • CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models . CB-5083 causes rapid and sustained accumulation of poly-ubiquitin in tumor xenografts after a single administration. CB-5083 showed activity to inhibit tumor growth in multiple rodent models of human cancer. Furthermore, CB-5083 appears to exhibit greater potency over current proteasome inhibitors that further validate targeting p97 and protein homeostasis in the treatment of cancer.

系列性分类

  1. Medical Research Areas
  2. Ubiquitin
  3. p97

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