Naphthofluorescein

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

Naphthofluorescein 抑制 HIF-1 和 Mint3 之间的相互作用。Naphthofluorescein 抑制 Mint3 依赖性 HIF-1 活性以及癌细胞和巨噬细胞的糖酵解活动，同时不引起体外细胞毒性和体内副作用。Naphthofluorescein 也是一种荧光 pH 敏感探针，可用于功能性切伦科夫成像。

Naphthofluorescein inhibits the interaction between HIF-1 and Mint3.Naphthofluorescein suppresses Mint3-dependent HIF-1 activity and glycolysis in cancer cells and macrophages without cytotoxicity in vitro and adverse effect in vivo. Naphthofluorescein is also a fluorescent pH-sensitive probe that can be used for functional Cerenkov imaging.

Naphthofluorescein (compound 19) (0-10 μM; 24 hours) suppresses the HIF-1 reporter activity in a concentration-dependent manner.Cell Viability Assay Cell Line:HT1080 cells Concentration:0-10 μM Incubation Time:24 hours Result:Significantly suppressed the HIF-1 reporter activity in a concentration-dependent manner.

Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks)does not show weight loss or apparent histological abnormalities in the lung, liver, and kidney, or cause cause severe adverse effects for at least 2 weeks in mice.Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks) strikingly suppresses the tumour growth of subcutaneously injected E0771 cells and significantly attenuates tumour growth of MDA-MB-231 and AsPC-1 cells in immunodeficient mice. In turn, naphthofluorescein does not attenuate tumour growth of FIH-1-depleted MDA-MB-231 cells.Naphthofluorescein (compound 19) (100 mg/kg; i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeks) suppresses tumour growth in human cancer cells in an FIH-1-dependent manner.Animal Model:Male C57BL/6J mice (8 weeks) Dosage:100 mg/kg Administration:i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeksResult:Neither showed weight loss or apparent histological abnormalities in the lung, liver, and kidney, or caused cause severe adverse effects for at least 2 weeks in mice.Animal Model:Female C57BL/6J mice (E0771) and BALB/c nude mice (HT1080, MDA-MB-231, and AsPC-1) (6 weeks) Dosage:100 mg/kg Administration:i.p.; once daily for 5 consecutive days followed by 2 days off for 2 weeksResult:Strikingly suppressed the tumour growth of subcutaneously injected E0771 cells and significantly attenuated tumour growth of MDA-MB-231 and AsPC-1 cells in immunodeficient mice. In turn, naphthofluorescein did not attenuate tumour growth of FIH-1-depleted MDA-MB-231 cells.

——

Angiogenesis

HIF/HIF Prolyl-hydroxylase

HIF

——

——

61419-02-1

432.42

C28H16O5

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (289.07 mM; 超声助溶 )

Oc1ccc2c3Oc4c(ccc5cc(O)ccc45)C4(OC(=O)c5ccccc45)c3ccc2c1

——

(-20℃)

With Ice Pack

≥ 2 years