产品
编 号：F749232
分子式：C27H20Cl2FNO2
分子量：480.36
分子式：C27H20Cl2FNO2
分子量：480.36
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CAS No: 2135341-09-0
产品详情
生物活性：
LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity.
体内研究：
LX-039 (2.5 mg/kg; PO and IV; single) exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure.LX-039 (6.5 mg/kg, 20 mg/kg and 60 mg/kg; PO; daily for 21 days) inhibits tumor growth in a dose-dependent manner.LX-039 (1 mg/kg; PO and IV; single) displays a moderate to low clearance (Cl) plus good oral bioavailability (F%) in both rat and dog.Pharmacokinetic Parameters of LX-039 in CD-1 mouse.IV PO (2.5 mg/kg)
Vd (L/kg)0.5
CL (mL/min/kg)1.4
Cmax (nM)1873
AUC0-24 (nM·h)15329
F (%)60.1
Pharmacokinetic Parameters of LX-039 in SD rat and Beagle dog.SD Rat Beagle Dog
Vd (L/kg, iv)20.42
CL (mL/min/kg, iv)7.70.84
C0, iv (nM), 1 mg/kg261012800
AUC0-24, iv (nM·h), 1 mg/kg482043800
Cmax, po (nM), 1 mg/kg3812550
AUC0-24, po (nM·h), 1 mg/kg270024200
F (%)5655
LX-039 is a highly potent, selective and orally active estrogen receptor degrader with EC50 value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure. LX-039 has anti-tumor activity.
体内研究：
LX-039 (2.5 mg/kg; PO and IV; single) exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure.LX-039 (6.5 mg/kg, 20 mg/kg and 60 mg/kg; PO; daily for 21 days) inhibits tumor growth in a dose-dependent manner.LX-039 (1 mg/kg; PO and IV; single) displays a moderate to low clearance (Cl) plus good oral bioavailability (F%) in both rat and dog.Pharmacokinetic Parameters of LX-039 in CD-1 mouse.IV PO (2.5 mg/kg)
Vd (L/kg)0.5
CL (mL/min/kg)1.4
Cmax (nM)1873
AUC0-24 (nM·h)15329
F (%)60.1
Pharmacokinetic Parameters of LX-039 in SD rat and Beagle dog.SD Rat Beagle Dog
Vd (L/kg, iv)20.42
CL (mL/min/kg, iv)7.70.84
C0, iv (nM), 1 mg/kg261012800
AUC0-24, iv (nM·h), 1 mg/kg482043800
Cmax, po (nM), 1 mg/kg3812550
AUC0-24, po (nM·h), 1 mg/kg270024200
F (%)5655
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