| Identification | Back Directory | [Name]
CB5083 | [CAS]
1542705-92-9 | [Synonyms]
CB5083
CB-5083
CS-1553
EOS-61078
CB 5083;CB5083
CB5083; CB-5083; CB 5083.
1-[4-(benzylamino)-5H,7H,8H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl-1H-indole-4-carboxamide
1-[4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methylindole-4-carboxamide
1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide
1H-Indole-4-carboxamide, 1-[7,8-dihydro-4-[(phenylmethyl)amino]-5H-pyrano[4,3-d]pyrimidin-2-yl]-2-methyl- | [Molecular Formula]
C24H23N5O2 | [MDL Number]
MFCD28963914 | [MOL File]
1542705-92-9.mol | [Molecular Weight]
413.47 |
| Chemical Properties | Back Directory | [Boiling point ]
760.5±70.0 °C(Predicted) | [density ]
1.37±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥20.65 mg/mL in DMSO; ≥4.4 mg/mL in EtOH | [form ]
solid | [pka]
15.99±0.30(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
CB-5083 is a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 AAA ATPase/VCP. CB-5083 selectively inhibits p97 through its D2 site with the IC50 of 11 nM[1]. | [Biological Activity]
cb-5083 is an orally bioavailable inhibitor of p97. p97 is an aaa-atpase involved in multiple cellular functions such as organelle membrane homotypic fusion and sorting of endosomal cargo. p97 is also known as valosin-containing protein which plays important roles in regulating protein homeostasis [1]. | [in vitro]
cb-5083 is a selective potent inhibitor of p97’s second atpase domain. cb-5083 might compete with atp for the same binding site but may adopt a different orientation[2]. the ic50 of cb-5083 against wild-type (wt) p97 was 15.4 nm. cb-5083 could dose-dependently increase the cytosolic protein degradation in hek293t, a549 and hct116 cell lines [1]. cb-5083 treatment (2.5 μm) of a549 cells for 24h could induce cancer cell death [1]. | [in vivo]
in female nude mice bearing hct116, a549 lung carcinoma, and amo-1 multiple myeloma xenograft tumors, oral administration of cb-5083 (100 mg/kg) for 6 h showed a significant antitumor response in tumors (tgi = 63%, p < 0.0001) [1,2]. | [IC 50]
15.4 nm | [storage]
Store at -20°C | [References]
anderson d j, le moigne r, djakovic s, et al. targeting the aaa atpase p97 as an approach to treat cancer through disruption of protein homeostasis[j]. cancer cell, 2015, 28(5): 653-665.zhou h j, wang j, yao b, et al. discovery of a first-in-class, potent, selective, and orally bioavailable inhibitor of the p97 aaa atpase (cb-5083)[j]. journal of medicinal chemistry, 2015, 58(24): 9480-9497. |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
|