2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. 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。

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LX-039 Chemical Structure

LX-039 Chemical Structure

CAS No. : 2135341-09-0

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LX-039 相关抗体

Top Publications Citing Use of Products

查看 Estrogen Receptor/ERR 亚型特异性产品:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

480.36

Formula

C27H20Cl2FNO2
CAS 号
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.
纯度 & 产品资料
参考文献

LX-039 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LX-0392135341-09-0LX039LX 039Estrogen Receptor/ERRBreast cancerTumorSelectiveOrally activeIndoleInhibitorinhibitorinhibit

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产品名称：
LX-039
目录号：
HY-143439
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