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
SMILES: Cc1cc2c(C(N)=O)cccc2n1-c1nc2c(c(NCc3ccccc3)n1)COCC2
化学属性
| Mol. Weight | 413.4 |
|---|
别名和识别编码
| PubChem Substance ID | 73051434 |
|---|---|
| InChI | InChI=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 Name | CB-5083 |
| Chemical Name Translation | 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 |
| Formula | C24H23N5O2 |
| IUPAC Name | 1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide |
| InChIKey | RDALZZCKQFLGJP-UHFFFAOYSA-N |
| Canonical SMILES | O=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.
