ZINC69391

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ZINC69391 是一种选择性 Rac1 抑制剂，具有抗增殖和抗转移作用。 ZINC69391 干扰 Rac1 与 Dock180 的相互作用，降低 Rac1-GTP 水平并诱导细胞凋亡。

ZINC69391 is a selective inhibitor of Rac1 with antiproliferative and antimetastatic effects. ZINC69391 interferes with the interaction of Rac1 with Dock180, reduces Rac1-GTP levels and induces apoptosis.(In Vitro):In U-87 MG and LN229 cells, ZINC69391 (0-125 μM) reduces cell proliferation of human glioma cells. ZINC69391 (50-100 μM) triggers cell cycle arrest. ZINC69391 inhibits the growth of U937, HL-60, KG1A, and Jurkat cells (IC50s = 41-54 μM). In HL-60, U937, and KG1A cell lines, ZINC69391 (50 μM) triggers an increase in apoptotic cells. In LN229 cells, ZINC69391 (50 and 100 μM) augments the enzymatic activity of caspase 3 and increases the percentage of cells in the sub-G0/G1 phase in a concentration-dependent manner.(In Vivo):In specific pathogen-free female BALB/c inbred mice (bearing F3II cells), ZINC69391 (25 mg/kg; i.p) impairs metastatic lung colonization and reduces by about 60% the formation of total metastatic lung colonies.

ZINC69391 inhibits growth of U937, HL-60, KG1A and Jurkat cells with IC50s ranging from 41 to 54 μM.ZINC69391 (50-100 μM; 24 hours) augments the enzymatic activity of caspase 3 in a concentration dependent manner.ZINC69391 (0-125 μM; 72h) reduces cell proliferation of human glioma cells.ZINC69391 (50-100 μM; 48 hours) triggers cell cycle arrest.ZINC69391 (50 μM; 24 hours) triggers apoptosis on human acute leukemic cells. Cell Proliferation Assay Cell Line:U-87 MG, LN229 cells Concentration:0-125μM Incubation Time:72 hours Result:Reduced cell proliferation in a concentration-dependent manner.Cell Cycle Analysis Cell Line:LN229 cells Concentration:50, 100 μM Incubation Time:48 hours Result:Resulted in a significant increased percentage of cells in the sub-G0/G1 phase in a concentration dependent manner.Apoptosis Analysis Cell Line:HL-60, U937 and KG1A cell lines Concentration:50 μM Incubation Time:24 hours Result:Led to a significant increase in apoptotic cells.

ZINC69391 (25 mg/kg; i.p; daily for 21 days) impairs metastatic lung colonization in a syngeneic animal model. Animal Model:Specific pathogen-free female BALB/c inbred mice (bearing F3II cells)Dosage:25 mg/kg body weight Administration:I.p; daily for 21 days Result:Significantly reduced by about 60% the formation of total metastatic lung colonies.

ZINC-69391 | N'-(4,6-dimethylpyrimidin-2-yl)-N-[2-(trifluoromethyl)phenyl]guanidine

Apoptosis

Apoptosis

EGFR|EGFR (L858R)|EGFR (L858R/T790M)|EGFR (L858R/T790M/C797S)

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303094-67-9

309.296

C14H14F3N5

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (80.83 mM)

Cc1cc(C)nc(NC(=N)Nc2ccccc2C(F)(F)F)n1

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(-20℃)

With Ice Pack

≥ 2 years