ChemicalBook > CAS DataBase List > CB-6644

CB-6644

Product Name
CB-6644
CAS No.
2316817-88-4
Chemical Name
CB-6644
Synonyms
Chb-M';CB-6644;CB-6644 (CB6644;CB-6644, 10 mM in DMSO;CB6644,CB-6644,Inhibitor,CB 6644,inhibit;5-Chloro-2-ethoxy-4-fluoro-N-(4-((3-(methoxymethyl)-1-oxo-6,7-dihydro-1H,5H-benzo[c]pyrazolo[1,2-a][1,2]diazepin-2-yl)amino)-2,2-dimethyl-4-oxobutyl)benzamide;Benzamide, 5-chloro-N-[4-[[6,7-dihydro-3-(methoxymethyl)-1-oxo-1H,5H-pyrazolo[1,2-a][1,2]benzodiazepin-2-yl]amino]-2,2-dimethyl-4-oxobutyl]-2-ethoxy-4-fluoro-
CBNumber
CB24844617
Molecular Formula
C29H34ClFN4O5
Formula Weight
573.06
MOL File
2316817-88-4.mol
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CB-6644 Property

Density 
1.34±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:100.0(Max Conc. mg/mL);174.5(Max Conc. mM)
form 
A solid
pka
13.13±0.20(Predicted)
color 
White to light yellow
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Hazard and Precautionary Statements (GHS)

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CB-6644 Chemical Properties,Usage,Production

Uses

CB-6644 is a selective inhibitor of RUVBL1/2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM[1].

Biological Activity

CB-6644 is a selective RUVBL1/2 complex inhibitor. It inhibits the ATPase activity of RUVBL1/2 with IC50 of 15 nM; it also has anticancer activity.

in vitro

CB-6644 (20 μM) interacts with the RUVBL1/2 complex in Ramos cells.
CB-6644 (0.001-10 μM; 72 hours) potently kills 123 cell lines (including HCT116, NCI -1975, and HT29 cells) with an EC 50 range of 41 to 785 nM.

Cell Viability Assay

Cell Line: 123 cell lines such as HCT116, NCI-1975, and HT29 cells
Concentration: 0.001, 0.01, 0.1, 1, and 10 μM
Incubation Time: 72 hours
Result: Potently killed cells with an EC 50 range of 41 to 785 nM.

in vivo

CB-6644 (150 mg/kg, oral administration, 10 days of treatment for SCID-beige mice bearing Ramos xenograft models, 30 days of treatment for SCID-beige mice bearing RPMI8226 xenograft models) has antitumor activity in xenograft tumor models with tumor growth inhibitions (TGIs) of 68 and 81%, respectively in Ramos xenograft models and RPMI8226 xenograft models.

Animal Model: SCID-beige mice bearing human tumor xenografts derived from either Burkitt's lymphoma (Ramos) or multiple myeloma (RPMI8226) cell lines
Dosage: < /td> 150 mg/kg
Administration: Oral gavage once (qd) or twice (BID) daily, 10 days of treatment for Ramos, 30 days of treatment for RPMI8226
Result: There was no significant bodyweight loss in mice. TGI of 68 and 81% in Ramos and RPMI8226, respectively.

References

[1] Assimon VA, et al. CB-6644 Is a Selective Inhibitor of the RUVBL1/2 Complex with Anticancer Activity. ACS Chem Biol. 2019 Feb 15;14(2):236-244. DOI:10.1021/acschembio.8b00904

CB-6644 Preparation Products And Raw materials

Raw materials

Preparation Products

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2316817-88-4, CB-6644Related Search:


  • CB-6644
  • CB-6644 (CB6644
  • Chb-M'
  • CB6644,CB-6644,Inhibitor,CB 6644,inhibit
  • Benzamide, 5-chloro-N-[4-[[6,7-dihydro-3-(methoxymethyl)-1-oxo-1H,5H-pyrazolo[1,2-a][1,2]benzodiazepin-2-yl]amino]-2,2-dimethyl-4-oxobutyl]-2-ethoxy-4-fluoro-
  • 5-Chloro-2-ethoxy-4-fluoro-N-(4-((3-(methoxymethyl)-1-oxo-6,7-dihydro-1H,5H-benzo[c]pyrazolo[1,2-a][1,2]diazepin-2-yl)amino)-2,2-dimethyl-4-oxobutyl)benzamide
  • CB-6644, 10 mM in DMSO
  • 2316817-88-4