LX-039

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LX-039 

LX-039 是一种高效、且具有选择性和口服活性的雌激素受体 (estrogen receptor) 降解剂,EC50 为 2.99 nM。LX-039 有吲哚 C-3 氯原子。LX-039 具有良好的小鼠药代动力学性质、低清除、高血药浓度和口服暴露率。具有抗肿瘤活性。

LX-039

LX-039 Chemical Structure

CAS No. : 2135341-09-0

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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[1].

IC50 & Target[1]

Estrogen receptor

2.29 nM (EC50)

体内研究
(In Vivo)

LX-039 (2.5 mg/kg; PO and IV; single) exhibits excellent mouse pharmacokinetics, low clearance, high Cmax and oral exposure[1].
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[1].
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[1].
Pharmacokinetic Parameters of LX-039 in CD-1 mouse[1].

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[1].

SD Rat Beagle Dog
Vd (L/kg, iv) 2 0.42
CL (mL/min/kg, iv) 7.7 0.84
C0, iv (nM), 1 mg/kg 2610 12800
AUC0-24, iv (nM·h), 1 mg/kg 4820 43800
Cmax, po (nM), 1 mg/kg 381 2550
AUC0-24, po (nM·h), 1 mg/kg 2700 24200
F (%) 56 55

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

480.36

Formula

C27H20Cl2FNO2

CAS 号

2135341-09-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Lu J, Chan CC, Sun D, et al. Discovery and preclinical profile of LX-039, a novel indole-based oral selective estrogen receptor degrader (SERD). Bioorg Med Chem Lett. 2022;66:128734.

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