LX-039

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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

Shanghai Jinpan Biotech Co Ltd 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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