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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- CAS No.: 925419-55-2
- Formule: C21H18BrNO3
- Masse moléculaire:412.28
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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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.
| Species | Dose | Route | Cmax |
|---|---|---|---|
| Mice[1] | 0.1 mg/kg | p.o. | 1.29 ng/mL |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 925419-55-2
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Masse moléculaire 412.28
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LNS8801 Related Classifications
HY-173178 Related Classifications
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- 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