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

BSJ-03-204 是由Cereblon配体和CDK配体相连的PROTAC，是一种有效的，选择性的基于 Palbociclib (HY-50767) 的 CDK4/6 双重降解剂，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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Customer Review

Other Forms of BSJ-03-204:

BSJ-03-204 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(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.

BSJ-03-204 相关抗体:

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.
分子量

832.90

Formula

C43H48N10O8
CAS 号
性状

固体

颜色

Light yellow to green yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light

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

纯度 & 产品资料
参考文献

BSJ-03-204 相关分类

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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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产品名称：
BSJ-03-204
目录号：
HY-136250
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