JH530 is an effective methuosis inducer that inhibits the triple-negative breast cancer (TNBC) cells proliferation by causing intracellular complete vacuolization. JH530 has anti-tumor activity and can be used for cancer research[1].
in vivo
JH530 (compound 5c ) (2.5 mg/kg or 5.0 mg/kg; i.p.; once every 2 days for two week) elicites tumor regression and well tolerated with treatment doses without causing a noticeable weight decrease[1].
Animal Model:
HCC1806 cell xenograft mouse model [1]
Dosage:
2.5 mg/kg, 5.0 mg/kg
Administration:
Intraperitoneal injection (i.p.); once every 2 days
Result:
Inhibits HCC1806 tumor weight at 2.5 mg/kg significantly, while exhibit more apparent tumor suppressive effects at 5 mg/kg[1].
References
[1] He J, et al. Discovery of Pyrimidinediamine Derivatives as Potent Methuosis Inducers for the Treatment of Triple-Negative Breast Cancer. J Med Chem. 2023 Jun 8;66(11):7421-7437. DOI:10.1021/acs.jmedchem.3c00090