LNS8801
LNS8801 is an orally active GPER activator with tumor suppressor activity. LNS8801 mediates suppression of cancer via GPER activation, with activity dependent on GPER expression. LNS8801 suppresses cancer growth in preclinical models. LNS8801 can be used for the research of cancer (including melanoma, pancreatic ductal adenocarcinoma, non-small cell lung cancer, leukemias, colon carcinomas).
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- No. CAS: 925419-55-2
- Fòrmula: C21H18BrNO3
- Peso molecular:412.28
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
Descripciòn
In Vitro
LNS8801 potently inhibits proliferation of YUMM1.7 murine melanoma cells and 2838c3 murine PDAC cells[1].
LNS8801 (0.1-10 μM; 15 min) induces dose-dependent cAMP production in HL-60 human promyelocytic leukemia cells, with significant activation starting at 1 μM[1].
LNS8801-induced cAMP production in HL-60 human promyelocytic leukemia cells is dependent on GPER expression[1].
LNS8801 (18 hours) induces CREB activity in wild-type primary human melanocytes, and this activity is dependent on GPER expression, as GPER depletion abolishes the response[1].
LNS8801 (18 hours)-induced CREB activity is attenuated in primary human melanocytes heterozygous for the Pro16Leu GPER variant (C/V) compared to melanocytes homozygous for the consensus GPER genotype (C/C)[1].
LNS8801 (up to 10 μM) has weak off-target activity at CNR1, HTR2A, OPRM1, and OPRD1, with all active concentrations far exceeding the plasma levels required for in vivo efficacy[1].
LNS8801 binds more strongly to GPER than its enantiomer LNS8812[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:YUMM1.7 (murine melanoma), 2838c3 (murine PDAC)
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Concentration:500 nM
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Incubation Time:4 days
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Result:Inhibited the proliferation of YUMM1.7 (murine melanoma), 2838c3 (murine PDAC).
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Cell Line:MP41, Omml.3 (uveal melanoma)
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Concentration:100 nM
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Incubation Time:24 h
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Result:Inhibited cell migration.
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Cell Line:92.1, Omml.3 (uveal melanoma)
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Concentration:500 nM
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Incubation Time:24 h
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Result:Induced G2-M phase arrest and increased sub-G1 population.
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Cell Line:U937, MOLM14 (AML)
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Concentration:250 nM
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Incubation Time:24 h
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Result:Induced XBP1 and CHOP expression.
Parmacokinetics
| Species | Dose | Route | Cmax |
|---|---|---|---|
| Mice[1] | 0.1 mg/kg | p.o. | 1.29 ng/mL |
In Vivo
LNS8801 (1 mg/kg; p.o; 3 consecutive days per week for 3 weeks) is efficacious when administered orally in 2838c3 PDAC-bearing mice, with comparable antitumor activity to subcutaneous administration[1].
LNS8801 (0.1 mg/kg; p.o; 3 consecutive days per week for 3 weeks) shows dose-dependent antitumor efficacy in 2838c3 PDAC-bearing mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J or NU/J (female, 5-7 weeks old, subcutaneous pancreatic ductal adenocarcinoma model)[1]
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Dosage:0.01 mg/kg (p.o.); 0.1 mg/kg (p.o.); 1 mg/kg (p.o.)
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Administration:p.o.; 3 consecutive days per week for 3 weeks; s.c.; 3 consecutive days per week for 3 weeks
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Result:Demonstrated significantly greater antitumor activity, including tumor clearance.
Reached antitumor effect saturation at the 0.1 mg/kg oral dose.
Achieved a maximum plasma concentration of 1.29 ng/mL on the third day following 3 consecutive days of 0.1 mg/kg oral dosing.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 925419-55-2
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Peso molecular 412.28
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Fòrmula C21H18BrNO3
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SMILES
BrC(C([C@@]1([H])NC(C=CC(C(C)=O)=C2)=C2[C@]3([H])[C@@]1([H])CC=C3)=C4)=CC5=C4OCO5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LNS8801 Related Classifications
HY-173178 Related Classifications
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Keywords
- LNS8801
- 925419-55-2
- LNS 8801
- LNS-8801
- Estrogen Receptor/ERR
- Apoptosis
- MDM-2/p53
- PAK
- colon carcinomas
- 2838c3 murine PDAC cells
- pancreatic ductal adenocarcinoma
- YUMM1.7 murine melanoma cells
- GPER
- leukemias
- G protein-coupled estrogen receptor
- HL-60 human promyelocytic leukemia cells
- non-small cell lung cancer
- melanoma
- Inhibitor
- inhibitor
- inhibit