Art. -Nr.: HY-145072

BSJ-01-175

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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.

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Reinheit: 99.88%
CAS. Nr.: 2227392-55-2
Formel: C₃₀H₃₃ClN₆O₂
Molecular Weight:545.08

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

BSJ-01-175 Chemical Structure

CAS. Nr.: 2227392-55-2

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Use of MCE Products

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CDK12

CDK13

Alle CDK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Kelly	IC₅₀	225.3 nM Compound: 22a; BSJ-01-175	Antiproliferative activity against human Kelly cells harboring CDK12 C1039F mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human Kelly cells harboring CDK12 C1039F mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 33945934]
Kelly	IC₅₀	42.2 nM Compound: 22a; BSJ-01-175	Antiproliferative activity against human Kelly cells harboring wild type CDK12 assessed as reduction in cell viability incubated for 72 hrs by CelTiter-Glo assay Antiproliferative activity against human Kelly cells harboring wild type CDK12 assessed as reduction in cell viability incubated for 72 hrs by CelTiter-Glo assay	[PMID: 33945934]

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.

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)	T_max (h)	C_max (ng/mL)	AUC_last (h•ng/mL)	T_1/2 (h)	CL (mL/min/kg)	V_SS (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.

Chemical Information

CAS. Nr. 2227392-55-2
Appearance Solid
Molecular Weight 545.08
Formel C₃₀H₃₃ClN₆O₂
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8346 mL

9.1730 mL

18.3459 mL

5 mM

0.3669 mL

1.8346 mL

3.6692 mL

10 mM

0.1835 mL

0.9173 mL

1.8346 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Jiang B, et al. Structure-activity relationship study of THZ531 derivatives enables the discovery of BSJ-01-175 as a dual CDK12/13 covalent inhibitor with efficacy in Ewing sarcoma. Eur J Med Chem. 2021;221:113481. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MCE Bioactive Compound Library

Alle CDK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BSJ-01-175 Related Classifications

HY-145072 Related Classifications