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

BSJ-03-204 is a PROTAC connected by ligands for Cereblon and CDK. 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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 531 In-stock
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10 mM * 1 mL in DMSO USD 531 In-stock
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1 mg USD 140 In-stock
5 mg USD 350 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of BSJ-03-204:

BSJ-03-204 Related Antibodies

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Customer Validation

These results were obtained using AlphaLISA™ SureFire® Ultra™ assays

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BSJ-03-204 is a PROTAC connected by ligands for Cereblon and CDK. 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].

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

BSJ-03-204 Related Antibodies

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.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C2CCCC2)C3=NC(NC4=CC=C(N(CC5)CCN5CCCCNC(COC6=C(C(N7C(CCC8=O)C(N8)=O)=O)C(C7=O)=CC=C6)=O)C=N4)=NC=C3C(C)=C1C(C)=O
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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.76%

SDS (252 KB)

COA (249 KB) HNMR (312 KB) RP-HPLC (259 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.2006 mL 6.0031 mL 12.0062 mL 30.0156 mL
5 mM 0.2401 mL 1.2006 mL 2.4012 mL 6.0031 mL
10 mM 0.1201 mL 0.6003 mL 1.2006 mL 3.0016 mL
15 mM 0.0800 mL 0.4002 mL 0.8004 mL 2.0010 mL
20 mM 0.0600 mL 0.3002 mL 0.6003 mL 1.5008 mL
25 mM 0.0480 mL 0.2401 mL 0.4802 mL 1.2006 mL
30 mM 0.0400 mL 0.2001 mL 0.4002 mL 1.0005 mL
40 mM 0.0300 mL 0.1501 mL 0.3002 mL 0.7504 mL
50 mM 0.0240 mL 0.1201 mL 0.2401 mL 0.6003 mL
60 mM 0.0200 mL 0.1001 mL 0.2001 mL 0.5003 mL
80 mM 0.0150 mL 0.0750 mL 0.1501 mL 0.3752 mL
100 mM 0.0120 mL 0.0600 mL 0.1201 mL 0.3002 mL
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BSJ-03-204 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BSJ-03-2042349356-09-6PROTACsCDKCyclin dependent kinasePalbociclibJeko-1MinoGranta-519Rec-1Maver-1mantlecelllymphomaMCLJurkatInhibitorinhibitorinhibit

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