LX-039

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LX-039

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2135341-09-0

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。

生物活性

LX-039 is a highly potent, selective and orally activeestrogen receptordegrader withEC₅₀value of 2.29 nM. LX-039 has indole C-3 chlorine atom. LX-039 exhibits excellent mouse pharmacokinetics, low clearance, high C_maxand 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 C_maxand 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
C_max(nM)		1873
AUC_0-24(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
AUC_0-24, iv (nM·h), 1 mg/kg	4820	43800
C_max, po (nM), 1 mg/kg	381	2550
AUC_0-24, po (nM·h), 1 mg/kg	2700	24200
F (%)	56	55

Clinical Trial

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.