1. Cell Cycle/DNA Damage
  2. p97

CB-5083 (Synonyms: CB5083; CB 5083)

Cat. No.: HY-12861 Purity: 99.49%
Data Sheet SDS Handling Instructions

CB-5083 is a potent, selective and orally bioavailable p97 inhibitor with an IC50 value of 11 nM.

For research use only. We do not sell to patients.
CB-5083 Chemical Structure

CB-5083 Chemical Structure

CAS No. : 1542705-92-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $110 In-stock
5 mg $100 In-stock
10 mg $140 In-stock
50 mg $400 In-stock
100 mg $750 In-stock
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500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CB-5083 is a potent, selective and orally bioavailable p97 inhibitor with an IC50 value of 11 nM.

IC50 & Target

IC50: 11 nM (p97)[1]

In Vitro

Treatment of tumor cells with CB-5083 leads to significant accumulation of markers associated with inhibition of ubiquitin−proteasome system and endoplasmic reticulum-associated degradation functions, which induces irresolvable proteotoxic stress and cell death[1]

In Vivo

In tumor bearing mice, oral administration of CB-5083 causes rapid accumulation of markers of the unfolded protein response and subsequently induces apoptosis leading to sustained antitumor activity in in vivo xenograft models of both solid and hematological tumors. CB-5083 has been taken into phase 1 clinical trials in patients with multiple myeloma and solid tumors[1].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02243917 Cleave Biosciences, Inc. Advanced Solid Tumors October 2014 Phase 1
NCT02223598 Cleave Biosciences, Inc. Lymphoid Hematological Malignancies|Relapsed and Refractory Multiple Myeloma July 2014 Phase 1
NCT02243917 Cleave Biosciences, Inc. Advanced Solid Tumors October 2014 Phase 1
NCT02223598 Cleave Biosciences, Inc. Lymphoid Hematological Malignancies|Relapsed and Refractory Multiple Myeloma July 2014 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.4186 mL 12.0928 mL 24.1856 mL
5 mM 0.4837 mL 2.4186 mL 4.8371 mL
10 mM 0.2419 mL 1.2093 mL 2.4186 mL
Kinase Assay
[1]

The ATPase assay is performed to determine the IC50 value. compounds (CB-5083) are diluted in DMSO with a 3-fold 10-point serial dilution starting at 10 μM. The assay is done in a 384-well plate with each row as a single dilution MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

A549 and other tumor cell lines are cultured according to ATCC guidelines. Cells are cultured in black or white, clear-bottomed, tissue culture-treated 384-well plates. Cells are treated with 10-point dose titration of the compound (CB-5083) in well duplicates. After a 72 h treatment, CellTiter-Glo is added to the white plates to measure cell viability[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mouse: Tumor-bearing mice are used to evaluate pharmacokinetics and pharmacodynamics effect and antitumor activity. Both molecules (CB-5083 and compoud 69) are administered orally as a suspension in 0.5% methylcellulose aqueous suspensions at the fixed dose strength of 150 mg/kg; plasma and tumor samples at multiple time points (2, 6, 16, and 24 h) are harvested for pharmacokinetics and pharmacodynamics analysis[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
M.Wt

413.47

Formula

C₂₄H₂₃N₅O₂

CAS No.

1542705-92-9

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.49%

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CB-5083
Cat. No.:
HY-12861
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