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

BSJ-01-175 

Cat. No.: HY-145072
Handling Instructions

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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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].

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) 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

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.
SMILES

ClC1=CN=C(N[[email protected]]2C[[email protected]@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

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

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BSJ-01-175
Cat. No.:
HY-145072
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