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Art. -Nr.: HY-P4144

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Onvitrelin ucalontide

(Synonyms: Phor18-LHRH (338613); EP-100)

Onvitrelin ucalontide (Phor18-LHRH (338613); EP-100) is a luteinizing hormone-releasing hormone (LHRH) receptor ligand. Onvitrelin ucalontide binds to functional LHRH receptors on cancer cells and mediates targeted cytotoxicity. Onvitrelin ucalontide reduces tumor volume, weight and the number of viable tumor cells in xenograft models. Onvitrelin ucalontide can be used for the research of breast cancer, ovarian cancer and prostate cancer.

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CAS. Nr.: 1174415-90-7
Formel: C₁₆₃H₂₄₃N₄₃O₃₂
Molecular Weight:3316.94

Speicherung:

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

Onvitrelin ucalontide Chemical Structure

CAS. Nr.: 1174415-90-7

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Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

Onvitrelin ucalontide (0.87 μM) potently inhibits the proliferation of human MDA-MB-435S.luc breast cancer cells, with an IC₅₀ of 0.87 μM^[1].
Onvitrelin ucalontide exhibits low acute hemolytic activity against human red blood cells (HA₅₀ = 297.9 μM), resulting in an IC₅₀/HA₅₀ ratio of 0.003^[1].
Onvitrelin ucalontide inhibits the proliferation of various human cancer cell lines, with its IC₅₀ values ranging from 0.86 μM (MDA-MB-435S.luc) to 11.8 μM (SKOV-3)^[1].
Onvitrelin ucalontide (0.0001-100 μM; 0.5-48 h) rapidly kills luteinizing hormone-releasing hormone (LHRH) receptor-positive human cancer cells (MDA-MB-435S, MCF-7, OVCAR-3, T47D, LNCaP) within 0.5-1 h, with an IC₅₀ value as low as 0.5 μM; it exhibits delayed activity in LHRH receptor-negative cells and shows high resistance in non-cancer cell lines^[1].
Onvitrelin ucalontide (2-10 μM; 5-30 minutes) specifically kills LHRH receptor-positive human MDA-MB-435S cancer cells within minutes by disrupting the plasma membrane, while exerting no effect on LHRH receptor-negative SKOV-3 cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:

human cancer cell lines (MDA-MB-435S, MCF-7, OVCAR-3, SKOV-3, T47D, LNCaP) and non-cancerous cell lines (MCF-10A, NIH:3T3)
Concentration:

0.0001-100 μM
Incubation Time:

0.5-48 h
Result:

Achieved maximal cytotoxic efficacy within 0.5-1 hour of incubation in LHRH receptor-positive cell lines: MDA-MB-435S had an IC₅₀ of 1.2 μM at 0.5 hours and 0.6 μM at 1 hour; MCF-7 had IC₅₀ values of 3.4-1.8 μM within 1 hour; OVCAR-3 had IC₅₀ values of 6.7 μM at 0.5 hours decreasing to 0.5 μM by 1 hour.
Showed delayed activity in LHRH receptor-negative SKOV-3, with maximal efficacy (IC₅₀ = 11.5 μM) achieved after 24 hours, matching the activity of the untargeted Phor18 (CLIP71).
Induced high resistance in non-cancerous cell lines, with IC₅₀ values >10 μM.

Cell Cytotoxicity Assay^[1]

Cell Line:

human MDA-MB-435S and SKOV-3 cancer cells
Concentration:

2-10 μM
Incubation Time:

5-30 minutes
Result:

Caused plasma membrane disintegration in LHRH receptor-positive MDA-MB-435S cells within 5 minutes at 10 μM.
Induced intracellular uptake, membrane blebbing, and vesicle formation in MDA-MB-435S cells within 30 minutes at 2 μM.
Showed no intracellular uptake, no membrane blebbing, and retained mitochondrial dye in LHRH receptor-negative SKOV-3 cells at 2 μM after 30 minutes.

In Vivo

Onvitrelin ucalontide (0.02-2 mg/kg; intravenous injection; administered a total of 3 times within 8 days) reduces tumor weight and the number of viable tumor cells in MDA-MB-435S.luc breast cancer xenografts^[1].
Onvitrelin ucalontide (0.00002-1 mg/kg; intravenous injection; once weekly; for 3 consecutive weeks) reduces the weight of MDA-MB-435S breast cancer xenografts^[1].
Onvitrelin ucalontide (2 mg/kg; intravenous injection; 3 doses administered over 14 days) induces tumor regression in multidrug-resistant OVCAR-3 ovarian cancer xenografts, reduces serum CA125 levels, and triggers tumor necrosis, with significant efficacy observable at doses as low as 0.2 mg/kg^[1].
Onvitrelin ucalontide (0.002-2 mg/kg; intravenous injection; administered a total of 3 times within 14 days) inhibits tumor growth of aggressive PC-3 prostate cancer xenografts and prevents tumor-induced weight loss, with significant efficacy observed even at a dose as low as 0.002 mg/kg^[1].

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

Animal Model:

Nu/Nu nude mice (female, 5 weeks old)^[1]
Dosage:

0.02 mg/kg; 0.2 mg/kg; 2 mg/kg
Administration:

i.v.; 3 total doses over 8 days
Result:

Decreased tumor weights and total live tumor cell counts significantly compared to saline control and (KKKFAFA)₃-LHRH control.
Achieved tumor weights similar to baseline at the 0.2 mg/kg dose.
Reduced tumor volumes significantly compared to baseline after 30 days post-treatment, with the smallest tumor volumes among LHRH conjugate groups.
Kept blood chemistry and complete blood count results within normal ranges, with no evidence of liver, kidney, or heart dysfunction; only a 1.5-fold elevation in potassium levels was noted.

Animal Model:

Nu/Nu nude mice (female, 5 weeks old)^[1]
Dosage:

0.00002 mg/kg; 0.0002 mg/kg; 0.002 mg/kg; 0.02 mg/kg; 0.2 mg/kg; 1 mg/kg
Administration:

i.v.; once per week; 3 weeks
Result:

Reduced tumor volumes and weights significantly compared to saline controls at the 0.0002 mg/kg dose and above.
Reduced tumor volume and weight significantly compared to baseline at 0.002 mg/kg and higher doses.
Induced significant tumor necrosis at doses as low as 0.0002 mg/kg, while saline control and untargeted CLIP71 + LHRH groups had viable tumor cells.

Animal Model:

Nu/Nu nude mice (female, 5 weeks old)^[1]
Dosage:

0.02 mg/kg; 0.2 mg/kg; 2 mg/kg
Administration:

i.v.; 3 total doses over 14 days
Result:

Reduced tumor volumes significantly compared to baseline at 0.2 mg/kg and 2 mg/kg.
Reduced tumor weights significantly compared to saline and untargeted CLIP71 controls at 0.2 mg/kg and 2 mg/kg, with tumor-free mice present in these dose groups.
Reduced serum CA125 levels significantly at 0.2 mg/kg and 2 mg/kg compared to saline controls.
Induced significant tumor necrosis, and reduced LHRH receptor levels in treated tumors by 1-2 score points.

Animal Model:

Nu/Nu nude mice (male, 6 weeks old)^[1]
Dosage:

0.002 mg/kg; 0.02 mg/kg; 0.2 mg/kg; 2 mg/kg
Administration:

i.v.; 3 total doses over 14 days
Result:

Decreased tumor volumes during treatment at all doses, with significant reductions compared to saline and untargeted CLIP71 controls observed at 0.002 mg/kg and above.
Reduced median tumor weights at necropsy significantly compared to saline and CLIP71 controls across all treated groups.
Maintained body weight in treated mice, while control mice experienced severe weight loss (>10 g) due to tumor burden.

Clinical Trial

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

Chemical Information

CAS. Nr. 1174415-90-7
Molecular Weight 3316.94
Formel C₁₆₃H₂₄₃N₄₃O₃₂
Synonyms

Phor18-LHRH (338613); EP-100
Sequence

Lys-Phe-Ala-Lys-Phe-Ala-Lys-Lys-Phe-Ala-Lys-Phe-Ala-Lys-Lys-Phe-Ala-Lys-Gln-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly
Sequence Shortening

KFAKFAKKFAKFAKKFAKQHWSYGLRPG
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 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)

Verweise

[1]. Carola Leuschner, et al. Lytic domain fusion constructs and methods of making and using same. WO2009094634A1. 2010-07-24.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

MOQ

Minimum order quantity

100 mg

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