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

BSJ-03-204 

目录号: HY-136250
产品使用指南

BSJ-03-204 是一种有效的,选择性的基于 Palbociclib (HY-50767) 的 CDK4/6 双重降解剂 (PROTAC),对 CDK4/D1 和 CDK6/D1 的 IC50 分别为 26.9 nM 和 10.4 nM。BSJ-03-204 不诱导 IKZF1/3 降解,具有抗癌活性。

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BSJ-03-204 Chemical Structure

BSJ-03-204 Chemical Structure

CAS No. : 2349356-09-6

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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].

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.

2349356-09-6

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

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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× = ×
C1   V1   C2   V2

Keywords:

BSJ-03-204PROTACCDKProteolysis-targeting chimeraCyclin dependent kinasePalbociclibJeko-1MinoGranta-519Rec-1Maver-1mantlecelllymphomaMCLJurkatInhibitorinhibitorinhibit

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BSJ-03-204
目录号:
HY-136250
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