1. PROTAC
    Cell Cycle/DNA Damage
  2. PROTAC
    CDK
  3. BSJ-03-204

BSJ-03-204 

Cat. No.: HY-136250 Purity: 98.34%
Handling Instructions

BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity.

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

BSJ-03-204 Chemical Structure

BSJ-03-204 Chemical Structure

CAS No. : 2349356-09-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 531 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 531 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

BSJ-03-204 is a potent and selective Palbociclib-based CDK4/6 dual degrader (PROTAC), with IC50s of 26.9 nM and 10.4 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 does not induce IKZF1/3 degradation and has anti-cancer activity[1].

IC50 & Target[1]

CDK4/D1

26.9 nM (IC50)

CDK6/D1

10.4 nM (IC50)

In Vitro

BSJ-03-204 (0.0001-100 μM; for 3 or 4 days) has potent anti-proliferative effects on MCL cell lines[1].
BSJ-03-204 (1 μM; for 1 day) potently induces a G1 arrest[1].
BSJ-03-204 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4/6 in WT cells, not IKZF1/3[1].

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

Cell Proliferation Assay[1]

Cell Line: MCL cell lines (Jeko-1, Mino, Granta-519, Rec-1, and Maver-1 cells)
Concentration: 0.0001-100 μM
Incubation Time: For 3 or 4 days
Result: Had potent anti-proliferative effects on mantle cell lymphoma (MCL) cell lines.

Cell Cycle Analysis[1]

Cell Line: Granta-519 cells
Concentration: 1 μM
Incubation Time: For 1 day
Result: Potently induced a G1 arrest.

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 CDK4/6 in WT cells, not IKZF1/3.
Molecular Weight

832.90

Formula

C₄₃H₄₈N₁₀O₈

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (120.06 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2006 mL 6.0031 mL 12.0062 mL
5 mM 0.2401 mL 1.2006 mL 2.4012 mL
10 mM 0.1201 mL 0.6003 mL 1.2006 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Product Name:
BSJ-03-204
Cat. No.:
HY-136250
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