1. PROTAC
    Cell Cycle/DNA Damage
  2. PROTACs
    CDK
  3. BSJ-04-132

BSJ-04-132 

Cat. No.: HY-136252 Purity: 98.08%
Handling Instructions

BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity.

For research use only. We do not sell to patients.

BSJ-04-132 Chemical Structure

BSJ-04-132 Chemical Structure

CAS No. : 2349356-39-2

Size Price Stock Quantity
5 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity[1].

IC50 & Target

CDK4/D1

50.6 nM (IC50)

CDK6/D1

30 nM (IC50)

In Vitro

BSJ-04-132 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4 in WT cells, not CDK6 and IKZF1/3[1].

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

Western Blot Analysis[1]

Cell Line: Wildtype (WT) or Crbn-/- Jurkat cells
Concentration: 0.1, 0.5, 1, 5 μM
Incubation Time: For 4 hours
Result: Only resulted in degradation of CDK4 in WT cells, not CDK6 and IKZF1/3.
Molecular Weight

819.91

Formula

C₄₂H₄₉N₁₁O₇

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (121.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2196 mL 6.0982 mL 12.1965 mL
5 mM 0.2439 mL 1.2196 mL 2.4393 mL
10 mM 0.1220 mL 0.6098 mL 1.2196 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (3.05 mM); Clear solution

  • 2.

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

    Solubility: 2.5 mg/mL (3.05 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (3.05 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
BSJ-04-132
Cat. No.:
HY-136252
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