2. Cell Cycle/DNA Damage
  3. CDK
  4. BSJ-01-175

BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells.

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

BSJ-01-175 Chemical Structure

BSJ-01-175 Chemical Structure

CAS No. : 2227392-55-2

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5 mg USD 820 In-stock
10 mg USD 1320 In-stock
25 mg USD 2650 In-stock
50 mg USD 4250 In-stock
100 mg USD 6800 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

BSJ-01-175 Related Antibodies

Top Publications Citing Use of Products

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

BSJ-01-175 is a potent and selective CDK12/13 covalent inhibitor. BSJ-01-175 demonstrates exquisite selectivity, potent inhibition of RNA polymerase II phosphorylation, and downregulation of CDK12-targeted genes in cancer cells[1].

IC50 & Target

CDK12

 

CDK13

 

In Vitro

BSJ-01–175 (0-10 μM; 72 hours) causes a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039[1].
BSJ-01–175 (0-10 μM; 72 hours) slightly decreases the activity of TC71 Ewing sarcoma cells compared to THZ531[1].
BSJ-01–175 (0-5 μM) specifically targets CDK12/13 and suppresses the transcription of BRAC1 and BRAC2[1].

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

BSJ-01-175 Related Antibodies

Cell Viability Assay[1]

Cell Line: Kelly wild type or CDK12C1039F cells
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Observed a 5-fold increase in cell viability compared to the wild type (WT), indicating strong dependence on covalent bond formation with Cys1039.

Cell Proliferation Assay[1]

Cell Line: TC71 Ewing sarcoma cells
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Slightly decreased the activity compared to THZ531.
In Vivo

BSJ-01–175 (10 mg/kg; i.p.; daily for 3 weeks) leads to a significant suppression of tumor growth throughout 3 weeks of drug treatment period[1].
Assessment of Pharmacokinetics (PK) profile of BSJ-01-175 in mouse[1].

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) AUClast (h•ng/mL) T1/2 (h) CL (mL/min/kg) VSS (L/kg) F (%)
IV 3 1511 1832 2.2 24.9 3.9
PO 10 2 272 1043 17

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

Animal Model: Female nude mice (BALB/c, 7-8 weeks) bearing TC71 Ewing sarcoma cells[1]
Dosage: 10 mg/kg
Administration: i.p.; daily for 3 weeks
Result: Led to a significant suppression of tumor growth throughout 3 weeks of drug treatment period.
Molecular Weight

545.08

Formula

C30H33ClN6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CN=C(N[C@H]2C[C@@H](CCC2)OC3=CC=C(C=C3)NC(/C=C/CN(C)C)=O)N=C1C4=CNC5=CC=CC=C45
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (183.46 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 1.8346 mL 9.1730 mL 18.3459 mL
5 mM 0.3669 mL 1.8346 mL 3.6692 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. 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (4.59 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (4.59 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. 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

Animal weight
(per animal)

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).
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.
Purity & Documentation
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. 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 1.8346 mL 9.1730 mL 18.3459 mL 45.8648 mL
5 mM 0.3669 mL 1.8346 mL 3.6692 mL 9.1730 mL
10 mM 0.1835 mL 0.9173 mL 1.8346 mL 4.5865 mL
15 mM 0.1223 mL 0.6115 mL 1.2231 mL 3.0577 mL
20 mM 0.0917 mL 0.4586 mL 0.9173 mL 2.2932 mL
25 mM 0.0734 mL 0.3669 mL 0.7338 mL 1.8346 mL
30 mM 0.0612 mL 0.3058 mL 0.6115 mL 1.5288 mL
40 mM 0.0459 mL 0.2293 mL 0.4586 mL 1.1466 mL
50 mM 0.0367 mL 0.1835 mL 0.3669 mL 0.9173 mL
60 mM 0.0306 mL 0.1529 mL 0.3058 mL 0.7644 mL
80 mM 0.0229 mL 0.1147 mL 0.2293 mL 0.5733 mL
100 mM 0.0183 mL 0.0917 mL 0.1835 mL 0.4586 mL
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BSJ-01-175 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-01-1752227392-55-2CDKCyclin dependent kinaseCDK12/13RNA polymerase II phosphorylationanti-cancerselectivecovalentEwing sarcomaInhibitorinhibitorinhibit

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