1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. LX-039

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.

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LX-039 Chemical Structure

LX-039 Chemical Structure

CAS No. : 2135341-09-0

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Description

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)

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

480.36

Formula

C27H20Cl2FNO2

CAS No.
SMILES

O=C(O)/C=C/C1=CC=C(/C(C(N2)=C(Cl)C3=C2C=CC=C3)=C(C4=CC=C(F)C=C4Cl)\CC)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • 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.

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LX-039
Cat. No.:
HY-143439
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