Obatoclax

Research use only, not for human use.

A potent inhibitor of Bcl-2 family with IC50s of 1-7 uM for Bcl-2, Bcl-XL, Bcl-w, Bcl-B, Mcl-1 and Bfl-1.

A potent inhibitor of Bcl-2 family with IC50s of 1-7 uM for Bcl-2, Bcl-XL, Bcl-w, Bcl-B, Mcl-1 and Bfl-1; potently interferes with the direct interaction between MCL-1 and BAK in intact mitochondrial outer membrane and inhibited the association between MCL-1 and BAK in intact cells.(In Vitro):Obatoclax Mesylate (GX15-070 Mesylate) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM.Obatoclax Mesylate (50-200 nM; 24-72 hours) induces a dose- and time-dependent reduction of cell numbers in all human colorectal cancer cell lines. In particular, the IC50 of cell proliferation at 72 h are 25.85, 40.69, and 40.01 nM for HCT116, HT-29, and LoVo cells, respectively.Obatoclax Mesylate (400 nM; for 24 hours) induces autophagy in OSCC cells.Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations.Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM.Obatoclax Mesylate induces T286 phosphorylation-dependent or -independent cyclin D1 degradation. in HCT116 and LoVo cells, the steady-state levels of p-Cyclin D (T286) began to decline once exposed to obatoclax Mesylate (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax Mesylate inhibits GSK3β but activates p38MAPK, while barely affecting ERK1/2 activity in HT-29 cells.Obatoclax Mesylate (50, 100, 150, 200, 250, 300, 350, 400, 450 nM) potently inhibits the clonogenic potential of oral cancer cells.(In Vivo):Obatoclax Mesylate (GX15-070 Mesylate; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner.

Obatoclax Mesylate (GX15-070 Mesylate) inhibits BCL-2, BCL-XL, MCL-1, BCL-w, A1, and BCL-b with Ki values≈1-7 μM. Obatoclax Mesylate (50-200 nM; 24-72 hours) induces a dose- and time-dependent reduction of cell numbers in all human colorectal cancer cell lines. In particular, the IC50 of cell proliferation at 72 h are 25.85, 40.69, and 40.01 nM for HCT116, HT-29, and LoVo cells, respectively. Obatoclax Mesylate (400 nM; for 24 hours) induces autophagy in OSCC cells. Obatoclax Mesylate (50-200 nM; for 24 hours) provokes a dose-dependent increase in the G1-phase cell populations.Obatoclax Mesylate (25-200 nM; for 24 hours) indicates a marked drop in cyclin D1 levels as low as 50 nM.Obatoclax Mesylate induces T286 phosphorylation-dependent or -independent cyclin D1 degradation.in HCT116 and LoVo cells, the steady-state levels of p-Cyclin D (T286) began to decline once exposed to obatoclax Mesylate (200 nM; 1, 3, 6, 12, 24 hours). Obatoclax Mesylate inhibits GSK3β but activates p38MAPK, while barely affecting ERK1/2 activity in HT-29 cells. Obatoclax Mesylate (50-450 nM) potently inhibits the clonogenic potential of oral cancer cells. Cell Proliferation AssayCell Line:human colorectal cancer HCT116, HT-29 and LoVo cells Concentration:50, 100, 200 nM Incubation Time:24, 48, and 72 hours Result:Induced a dose- and time-dependent reduction of cell numbers.Cell Autophagy Assay Cell Line:AW8507 and SCC029B cells Concentration:400 nM Incubation Time:24 hours Result:Induced autophagy in OSCC cells.Cell Cycle Analysis Cell Line:HCT116 and HT-29 cells Concentration:50, 100, 200 nM Incubation Time:24 hours Result:Provoked a dose-dependent increase in the G1-phase cell populations. Western Blot Analysis Cell Line:HCT116, HT-29 and LoVo cells Concentration:25, 50, 100, 200 nM Incubation Time:24 hours Result:Indicated a marked drop in cyclin D1 levels as low as 50 nM.

Obatoclax Mesylate (GX15-070 Mesylate; 1.15-5 mg/kg; intravenously injected; five consecutive days) exhibits potent antitumor activity in xenograft mouse models in a dose-dependent manner. Animal Model:6-8 weeks old female BALB/C nude mice bearing subcutaneous tumors Dosage:1.15, 2.5, 5 mg/kg Administration:Intravenously injected (through lateral tail vein); five consecutive days (i.e. 5 injections) Result:Exhibited potent antitumor activity in xenograft mouse models in a dose-dependent manner.

Obatoclax Mesylate | GX15-070

Angiogenesis

Bcl-2

Bcl-2

Cancer

——

803712-79-0

413.49

C21H23N3O4S

>98% (HPLC)

DMSO: ≥ 48.8 mg/mL

CC1=CC(=C(N1)/C=C\2/C(=C/C(=C/3\C=C4C=CC=CC4=N3)/N2)OC)C.CS(=O)(=O)O

1H-Indole, 2-[2-[(3,5-dimethyl-1H-pyrrol-2-yl)methylene]-3-methoxy-2H-pyrrol-5-yl]-, methanesulfonate (1:1)

(-20℃)

With Ice Pack

≥ 2 years