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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- CAS. Nr.: 2135341-09-0
- Formel: C27H20Cl2FNO2
- Molecular Weight:480.36
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Estrogen receptor 2.29 nM (EC50) |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2135341-09-0
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Molecular Weight 480.36
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Formel C27H20Cl2FNO2
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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
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
LX-039 Related Classifications
HY-143439 Related Classifications
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