CB-5083, p97 AAA ATPase Inhibitor
Product Name :
CB-5083, p97 AAA ATPase Inhibitor
Description:
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.
CAS:
1542705-92-9
Molecular Weight:
413.47
Formula:
C24H23N5O2
Chemical Name:
1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide
Smiles :
CC1=CC2C(=CC=CC=2C(N)=O)N1C1=NC2CCOCC=2C(NCC2C=CC=CC=2)=N1
InChiKey:
RDALZZCKQFLGJP-UHFFFAOYSA-N
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)
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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.|Product information|CAS Number: 1542705-92-9|Molecular Weight: 413.47|Formula: C24H23N5O2|Chemical Name: 1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide|Smiles: CC1=CC2C(=CC=CC=2C(N)=O)N1C1=NC2CCOCC=2C(NCC2C=CC=CC=2)=N1|InChiKey: RDALZZCKQFLGJP-UHFFFAOYSA-N|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)|Technical Data|Appearance: Solid Power.{{Carbamazepine} web|{Carbamazepine} Sodium Channel|{Carbamazepine} Technical Information|{Carbamazepine} In Vitro|{Carbamazepine} manufacturer|{Carbamazepine} Cancer} |Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 100 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Biotin-PEG4-NHS ester} web|{Biotin-PEG4-NHS ester} PROTAC Linkers|{Biotin-PEG4-NHS ester} Epigenetics|{Biotin-PEG4-NHS ester} Protocol|{Biotin-PEG4-NHS ester} References|{Biotin-PEG4-NHS ester} supplier} |Shelf Life: ≥12 months if stored properly.PMID:24914310 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|CB-5083 was used at 1-2.5 µM final concentration in various assays.|In Vivo:|CB-5083 was dosed to mice orally at 25-100 mg/Kg once or twice per day.|References:|Zhou HJ, et al. Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083). (2015) J Med Chem. 58(24):9480-97.Products are for research use only. Not for human use.|Documents||