Onvitrelin ucalontide
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 No.: 1174415-90-7
- Formule: C163H243N43O32
- Masse moléculaire:3316.94
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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.
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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)
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Concentration:0.0001-100 μM
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Incubation Time:0.5-48 h
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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.
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Cell Line:human MDA-MB-435S and SKOV-3 cancer cells
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Concentration:2-10 μM
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Incubation Time:5-30 minutes
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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.
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.
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Animal Model:Nu/Nu nude mice (female, 5 weeks old)[1]
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Dosage:0.02 mg/kg; 0.2 mg/kg; 2 mg/kg
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Administration:i.v.; 3 total doses over 8 days
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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.
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Animal Model:Nu/Nu nude mice (female, 5 weeks old)[1]
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Dosage:0.00002 mg/kg; 0.0002 mg/kg; 0.002 mg/kg; 0.02 mg/kg; 0.2 mg/kg; 1 mg/kg
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Administration:i.v.; once per week; 3 weeks
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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.
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Animal Model:Nu/Nu nude mice (female, 5 weeks old)[1]
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Dosage:0.02 mg/kg; 0.2 mg/kg; 2 mg/kg
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Administration:i.v.; 3 total doses over 14 days
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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.
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Animal Model:Nu/Nu nude mice (male, 6 weeks old)[1]
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Dosage:0.002 mg/kg; 0.02 mg/kg; 0.2 mg/kg; 2 mg/kg
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Administration:i.v.; 3 total doses over 14 days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1174415-90-7
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Masse moléculaire 3316.94
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Formule C163H243N43O32
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Synonyms
Phor18-LHRH (338613); EP-100
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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
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Sequence Shortening
KFAKFAKKFAKFAKKFAKQHWSYGLRPG
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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)
Onvitrelin ucalontide Related Classifications
HY-P4144 Related Classifications
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- Onvitrelin ucalontide
- 1174415-90-7
- Phor18-LHRH (338613)
- EP-100
- EP100
- EP 100
- EP-100
- GnRH Receptor
- plasma membranes
- breast cancer
- MDA-MB-435S.luc breast cancer cells
- human red blood cells
- luteinizing hormone-releasing hormone (LHRH) receptor
- ovarian cancer
- xenograft models
- necrotic cell death
- cancer cells
- prostate cancer
- Inhibitor
- inhibitor
- inhibit