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

BSJ-03-204 is a PROTAC linking a Cereblon ligand to a CDK ligand, serving as a potent and selective dual degrader of CDK4/6. BSJ-03-204 exhibits IC50 values of 26.9 nM and 10.4 nM against CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 can be utilized for cancer-related research.
(Pink: Cdk4/cyclin D1 and Cdk6/cyclin D2 ligand (HY-50767); Blue: Cereblon ligand (HY-103596); Black: linker (HY-W007803)).

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CAS 番号 : 2349356-09-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 641 在庫あり
Solution
10 mM * 1 mL in DMSO USD 641 在庫あり
Solid
1 mg $140 在庫あり
5 mg $350 在庫あり
10 mg $580 在庫あり
25 mg $1100 在庫あり
50 mg $1700 在庫あり
100 mg $2500 在庫あり
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Based on 0 publication(s) in Google Scholar

Other Forms of BSJ-03-204:

BSJ-03-204 関連抗体

Top Publications Citing Use of Products

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

CDK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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  • 純度とドキュメンテーション

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製品説明

BSJ-03-204 is a PROTAC linking a Cereblon ligand to a CDK ligand, serving as a potent and selective dual degrader of CDK4/6. BSJ-03-204 exhibits IC50 values of 26.9 nM and 10.4 nM against CDK4/D1 and CDK6/D1, respectively. BSJ-03-204 can be utilized for cancer-related research[1]. (Pink: Cdk4/cyclin D1 and Cdk6/cyclin D2 ligand (HY-50767); Blue: Cereblon ligand (HY-103596); Black: linker (HY-W007803)).

IC50 & Target[1]

CDK4/D1

26.9 nM (IC50)

CDK6/D1

10.4 nM (IC50)

体外実験

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 関連抗体

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

分子式

C43H48N10O8
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

-20°C, protect from light

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

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
10 mM 0.1201 mL 0.6003 mL 1.2006 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.76%

COA (247 KB) HNMR (312 KB) RP-HPLC (259 KB) LCMS (95 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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製品名:
BSJ-03-204
製品番号:
HY-136250
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