产品
编 号:F755413
分子式:C23H29NO6
分子量:415.48
产品类型
结构图
CAS No: 2756173-91-6
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生物活性:
CHNQD-01255 is an orally active Arf-GEFs inhibitor with potent anti-hepatocellular carcinoma (HCC) efficacy.
体内研究:
CHNQD-01255 (5- 45 mg/kg, p.o.) inhibits tumor growth in HepG2 tumor-bearing xenograft mice.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.Animal Model:HepG2 tumor-bearing xenograft mice
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
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)
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.)7.3520.26598245.372.26
10 (i.v.) 2060.78
体外研究:
CHNQD-01255 (0-1 μM approximately, 72 h) inhibits HepG2 and BEL-7402 cell proliferation.