1. Cell Cycle/DNA Damage
  2. p97
  3. CB-5083

CB-5083 

Cat. No.: HY-12861 Purity: 99.90%
Handling Instructions

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。

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  
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 55 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    CB-5083 purchased from MCE. Usage Cited in: Leukemia. 2019 Jul;33(7):1675-1686.

    Jeko-1 and Z138C cells are exposed to the indicated concentrations of CB-5083 and ACY-1215 in the presence or absence of the autophagy inhibitor chloroquine for 6 h and LC3B-II and p62 expression is assessed by immunoblot analysis.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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]

    IC50 & Target

    IC50: 11 nM (p97)[1]

    In Vitro

    CB-5083 shows cell killing potency with IC50s of 0.68, 0.68, 1.03, and 0.49 μM for lung carcinoma A549 CTG, A549 K48, A549 CHOP, and A549 p62, respectively[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    In Vivo

    CB-5083 (75 mg/kg; oral administration; qd; for 2 weeks) shows antitumor activity in an HCT 116 tumor xenograft model[1].
    CB-5083 exhibits terminal elimination half-life (T1/2=2.56 h), moderate oral bioavailability (mouse 41%) and Cmax (mouse 7.95 μM) following oral administration (25 mg/kg) in female nude mice[1].
    CB-5083 exhibits terminal elimination half-life (T1/2=2.83 h) due to high plasma clearance (5.9 mL/min/kg respectively) combined with large volumes of distribution (418 mL/kg respectively) following intravenous administration (3.0 mg/kg) in female nude mice[1].
    CB-5083 has good metabolic stability with a 102 min T1/2 in a mouse liver microsomal stability study and a 172 min T1/2 in a hepatocyte stability study[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Nu/Nu nude female mice bearing established human tumor xenografts derived from HCT 116 colon[1]
    Dosage: 75 mg/kg
    Administration: Administered orally using every day (qd) dosing, for 2 weeks.
    Result: Showed more profound antitumor activity.
    Clinical Trial
    Molecular Weight

    413.47

    Formula

    C₂₄H₂₃N₅O₂

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (241.86 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  50% PEG300    50% saline

      Solubility: 10 mg/mL (24.19 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.05 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.90%

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    Product Name:
    CB-5083
    Cat. No.:
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