MI-1061

小分子

MI-1061

M656173-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor ( IC 50 =4.4 nM; K i =0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity In Vitro MI-1061 achieves IC 50 =100 and 250 nM in the SJSA-1 and HCT-116 p53 +/+ cell lines, respectively, and has IC 50 >10000 nM in the p53 knockout cell line HCT-116 p53 –/– cell line. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo MI-1061 (100 mg/kg; p.o.; daily for 14 days) is capable of achieving tumor regression in the SJSA-1 xenograft tumor model in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice bearing SJSA-1 osteosarcoma xenografts Dosage: 100 mg/kg Administration: P.o.; daily for 14 days Result: Demonstrated strong antitumor activity and achieved significant tumor regression. IC50& Target:IC50: 4.4 nM (MDM2),Ki: 0.16 nM (MDM2)

MI-1061 是一种强效、口服生物利用度高、化学性质稳定的 MDM2（MDM2-p53 相互作用）抑制剂（IC 50 =4.4 nM；K i =0.16 nM）。MI-1061 能有效激活 p53 并诱导小鼠 SJSA-1 异种移植肿瘤组织凋亡。抗肿瘤活性 [1

1410737-34-6(DMSO)

C30H26Cl2FN3O4

582.45 g/mol

C1CCC2(CC1)C3(C(C(N2)C(=O)NC4=CC=C(C=C4)C(=O)O)C5=C(C(=CC=C5)Cl)F)C6=C(C=C(C=C6)Cl)NC3=O