LLL12

Product NameLLL12
CAS1260247-42-4
MFC14H9NO5S
MW303.29
EINECS
MOL File1260247-42-4.mol

Chemical Properties

Melting point	179-181 °C
Boiling point	618.2±65.0 °C(Predicted)
Density	1.626±0.06 g/cm3(Predicted)
pka	6.46±0.20(Predicted)
form	Solid
color	Light yellow to yellow

Usage And Synthesis

Description

LLL12 is a potent STAT3 inhibitor. LLL12 inhibits colony formation and cell migration and works synergistically with doxorubicin and gemcitabine. LLL12 demonstrated a potent inhibitory activity on breast and glioblastoma tumor growth in a mouse xenograft model. LLL12 may be a potential therapeutic agent for human cancer cells expressing constitutive STAT3 signaling.

Uses

LLL12 is a small molecule inhibitor of STAT3 that inhibits STAT3 phosphorylation. LLL12 enhanced the inhibitory effect of Cisplatin (HY-17394) and Paclitaxel (HY-B0015) on ovarian cancer cell formation, migration, and growth[1].

in vivo

LLL12 (5 mg/kg; i.p.; once daily for 13 d) shows strong growth inhibition activity in mouse osteosarcoma cells and tumor growth^[2].

Animal Model:	Mouse xenografts with SJSA or OS-33 osteosarcoma cells^[2]
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; once daily for 13 days
Result:	Resulted in a significant reduction in tumor volume and tumor mass in the OS-33 and SJSA xenografted mice.

IC 50

p-STAT3

References

[1] Zhang R, et al. A small molecule STAT3 inhibitor, LLL12, enhances cisplatin and paclitaxelmediated inhibition of cell growth and migration in human ovarian cancer cells. Oncol Rep. 2020 Sep;44(3):1224-1232. DOI:10.3892/or.2020.7667
[2] Onimoe GI, et al. Small molecules, LLL12 and FLLL32, inhibit STAT3 and exhibit potent growth suppressive activity in osteosarcoma cells and tumor growth in mice. Invest New Drugs. 2012 Jun;30(3):916-26. DOI:10.1007/s10637-011-9645-1