For research use only. Not for therapeutic Use.
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].
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].
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
| Catalog Number | I045186 |
| CAS Number | 2227392-55-2 |
| Synonyms | (E)-N-[4-[(1R,3R)-3-[[5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl]amino]cyclohexyl]oxyphenyl]-4-(dimethylamino)but-2-enamide |
| Molecular Formula | C30H33ClN6O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C30H33ClN6O2/c1-37(2)16-6-11-28(38)34-20-12-14-22(15-13-20)39-23-8-5-7-21(17-23)35-30-33-19-26(31)29(36-30)25-18-32-27-10-4-3-9-24(25)27/h3-4,6,9-15,18-19,21,23,32H,5,7-8,16-17H2,1-2H3,(H,34,38)(H,33,35,36)/b11-6+/t21-,23-/m1/s1 |
| InChIKey | DMUSMYYDKCXFKR-MRJIRHQNSA-N |
| SMILES | CN(C)CC=CC(=O)NC1=CC=C(C=C1)OC2CCCC(C2)NC3=NC=C(C(=N3)C4=CNC5=CC=CC=C54)Cl |
| Reference | [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. |
