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Cat. No.: HY-173178

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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
화학식: C₂₁H₁₈BrNO₃
분자량:412.28

보관:

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

Data Sheet (287 KB)

LNS8801 Chemical Structure

CAS No.: 925419-55-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

All Estrogen Receptor/ERR Isoforms :

All PAK Isoforms :

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.

Cell Proliferation Assay^[1]

Cell Line:

YUMM1.7 (murine melanoma), 2838c3 (murine PDAC)
Concentration:

500 nM
Incubation Time:

4 days
Result:

Inhibited the proliferation of YUMM1.7 (murine melanoma), 2838c3 (murine PDAC).

Cell Migration Assay^[3]

Cell Line:

MP41, Omml.3 (uveal melanoma)
Concentration:

100 nM
Incubation Time:

24 h
Result:

Inhibited cell migration.

Cell Cycle Analysis^[3]

Cell Line:

92.1, Omml.3 (uveal melanoma)
Concentration:

500 nM
Incubation Time:

24 h
Result:

Induced G2-M phase arrest and increased sub-G1 population.

Western Blot Analysis^[4]

Cell Line:

U937, MOLM14 (AML)
Concentration:

250 nM
Incubation Time:

24 h
Result:

Induced XBP1 and CHOP expression.

Parmacokinetics

Species	Dose	Route	C_max
Mice^[1]	0.1 mg/kg	p.o.	1.29 ng/mL

In Vivo

LNS8801 (1 mg/kg; s.c.; 3 consecutive days per week for 3 weeks) suppresses tumor growth and improves survival in 2838c3 PDAC-bearing mice^[1].
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.

Animal Model:

C57BL/6J or NU/J (female, 5-7 weeks old, subcutaneous pancreatic ductal adenocarcinoma model)^[1]
Dosage:

0.01 mg/kg (p.o.); 0.1 mg/kg (p.o.); 1 mg/kg (p.o.)
Administration:

p.o.; 3 consecutive days per week for 3 weeks; s.c.; 3 consecutive days per week for 3 weeks
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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 925419-55-2
분자량 412.28
화학식 C₂₁H₁₈BrNO₃
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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Natale CA, et al. An enantiomerically pure agonist of the G protein-coupled estrogen receptor suitable for clinical development. bioRxiv [Preprint]. 2024 Dec 1:2024.11.26.625421.

[2]. Natale CA, et al. LNS8801: An enantiomerically pure agonist of the G protein-coupled estrogen receptor suitable for clinical development. bioRxiv [Preprint]. 2024 Dec 1:2024.11.26.625421.

[3]. Ambrosini G, et al. The GPER Agonist LNS8801 Induces Mitotic Arrest and Apoptosis in Uveal Melanoma Cells. Cancer Res Commun. 2023 Apr 5;3(4):540-547.

[4]. Carolyn Muller, et al. Phase 1 trial of a novel, first-in-class G protein-coupled estrogen receptor (GPER) agonist, LNS8801, in patients with advanced or recurrent treatment-refractory solid malignancies.. J Clin Oncol 39, 3084-3084(2021).

[5]. Carolyn Muller, et al. Phase 1b study of the novel first-in-class G protein-coupled estrogen receptor (GPER) agonist, LNS8801, in combination with pembrolizumab in patients with immune checkpoint inhibitor (ICI)-relapsed and refractory solid malignancies and dose escalation update.. J Clin Oncol 40, 2574-2574(2022).

[6]. Lee I, et al. LNS8801 inhibits Acute Myeloid Leukemia by Inducing the Production of Reactive Oxygen Species and Activating the Endoplasmic Reticulum Stress Pathway. Cancer Res Commun. 2023 Aug 18;3(8):1594-1606.

Calculators

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biological Activity
- 제품 설명
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
순도&문서
References

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LNS8801

All Estrogen Receptor/ERR Isoforms

All PAK Isoforms