| Description |
CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy[1].
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| Related Catalog |
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| In Vitro |
CHNQD-01255 (0-1 μM approximately, 72 h) inhibits HepG2 and BEL-7402 cell proliferation[1]. Cell Proliferation AssayCHNQD-01255 (0-1 μM approximately, 72 h) inhibits HepG2 and BEL-7402 cell proliferation[1]. Cell Line: HepG2, BEL-7402 cell Concentration: 0-1 μM approximately Incubation Time: 72 h Result: Inhibited cell proliferation with an IC50 value of 0.1 μM (HepG2) and 0.07 μM (BEL-7402).
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| In Vivo |
CHNQD-01255 (5- 45 mg/kg, p.o.) inhibits tumor growth in HepG2 tumor-bearing xenograft mice[1]. CHNQD-01255 exhibits a high safety profile with MTD values exceeding 750 and 100 mg/kg for p.o. and i.p. administrations in mice[1]. Animal Model: HepG2 tumor-bearing xenograft mice[1] Dosage: 5, 15, and 45 mg/kg Administration: Oral adminstration (p.o.), every day for 21 consecutive days. Result: Resulted in dramatically delayed tumor progression, with a tumor growth inhibition rate (TGI %) value of 61.0% at 45 mg/kg. Animal Model: HepG2 tumor-bearing xenograft mice[1] Dosage: 1 and 9 mg/kg Administration: Intraperitoneal injection (i.p.), every day for 21 consecutive days. Result: Inhibited the tumor growth with the TGI values of 36.6 and 48.3%, respectively. Animal Model: Mice (Pharmacokinetic assay)[1] Dosage: 45 mg/kg p.o., 10 mg/kg i.v. Administration: Oral adminstration (p.o.) or intravenous injection (i.v.) Result: Pharmacokinetic profile of CHNQD-01255. dose (mg/kg) T1/2 (h) Cmax (ng/mL) Cl (mL/h/kg) F (%) 45 (p.o.) 7.35 20.26 598245.37 2.26 10 (i.v.) 2060.78
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| References |
[1]. Yao-Yao Jiang, et al. Design and Characterization of a Natural Arf-GEFs Inhibitor Prodrug CHNQD-01255 with Potent Anti-Hepatocellular Carcinoma Efficacy In Vivo. J Med Chem. 2022 Sep 22;65(18):11970-11984.
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