| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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Purity: ≥98%
Cetrorelix mono-acetate (SB-75) is a novel, potent and synthetic gonadotropin-releasing hormone (GnRH) receptor antagonist with an IC50 of 1.21 nM. Cetrorelix acetate is a decapeptide that may be applied to the treatment of infertility. An autocrine regulatory system of cell proliferation has been shown to be triggered by the expression of GnRH (GnRH-I, LHRH) and its receptor in a variety of human malignant tumors, including ovarian cancers. GnRH and its superagonistic analogs decrease the proliferation of human ovarian cancer cell lines in a dose- and time-dependent manner.
| Targets |
GnRH ( IC50 = 1.21 nM )
Cetrorelix acetate (SB-75) is a GnRH-I (LHRH) receptor antagonist. [2] |
|---|---|
| ln Vitro |
Cetrorelix Acetate inhibits the growth of the ES-2 cell line at 1000 ng/ml. The antiproliferative effects of Cetrorelix Acetate are similar to those of GnRH-I agonists, suggesting that the GnRH-I system in cancer cells may not be subject to the GnRH-I agonists and antagonists dichotomy[2].
Cetrorelix acts as an antagonist of the GnRH-I receptor and inhibits the proliferation of human ovarian cancer cell lines in a dose- and time-dependent manner, comparable to the effects of GnRH-I agonists in most cell lines except EFO-27. [2] Cetrorelix inhibits epidermal growth factor (EGF)-induced c-fos expression in human gynecological cancer cells. [2] In the ES-2 ovarian cancer cell line, Cetrorelix inhibited cell growth only at a high concentration of 1000 ng/ml. [2] After GnRH-I receptor knockdown in EFO-21 and OVCAR-3 ovarian cancer cell lines, the antiproliferative effects of GnRH-I agonist Triptorelin were abolished, while the effects of Cetrorelix and GnRH-II persisted, suggesting that its antiproliferative action is not mediated through the classical GnRH-I receptor. [2] |
| ln Vivo |
In a study using the human ovarian cancer cell line OV-1063 xenografted into nude mice, chronic treatment with Cetrorelix significantly inhibited tumor growth, whereas the GnRH-I agonist Triptorelin did not. Since both analogs comparably suppressed the pituitary-gonadal axis, the antitumor effect of Cetrorelix was suggested to be mediated directly through tumor GnRH-I receptors. [2]
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| Cell Assay |
Cell proliferation was assessed using methods such as MTT assay or direct cell counting after treatment with varying concentrations of Cetrorelix. [2]
Western blot analysis and immunofluorescence were used to evaluate protein expression changes (e.g., c-fos, growth factor receptors) following Cetrorelix treatment. [2] To study signaling mechanisms, cells were stimulated with EGF after pretreatment with Cetrorelix, and downstream effects on mitogenic signaling pathways were analyzed. [2] |
| Animal Protocol |
In the referenced xenograft study (Yano et al.), nude mice bearing OV-1063 human epithelial ovarian cancer tumors were treated chronically with Cetrorelix. The specific dose, formulation, frequency, and route of administration for Cetrorelix are not detailed in this review article. [2]
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| References | |
| Additional Infomation |
Cetrorelix acetate is the acetate salt of cetrorelix. It is a gonadotropin-releasing hormone (GnRH) antagonist used to treat infertility and hormone-sensitive prostate and breast cancer. It is both a GnRH antagonist and an anti-tumor drug. It is an oligopeptide and also an acetate. It contains the cetrorelix molecule.
See also: Cetrorelix acetate (note moved to). Drug Indications Prevention of premature ovulation in patients undergoing controlled ovarian stimulation, oocyte retrieval, and assisted reproductive technologies. In clinical trials, cetrorelix has been used in combination with human menopausal gonadotropin (HMG), but limited experience with recombinant follicle-stimulating hormone (FSH) suggests similar efficacy. Cetrolix is a GnRH-I antagonist. Unlike its classic antagonistic effect in the pituitary gland, it exhibits similar antiproliferative activity to GnRH-I agonists in many human ovarian cancer cells, suggesting that the agonist/antagonist dichotomy may not apply to cancer cells. [2] The antiproliferative effect of cetrorelix in ovarian cancer cells appears to be independent of the classic GnRH-I receptor signaling pathway, possibly involving interaction with the putative GnRH-II receptor or acting through other mechanisms. [2] Cetrolix has been shown to have direct in vivo antitumor activity in ovarian cancer xenograft models, supporting its potential as a targeted therapy beyond endocrine action. [2] |
| Molecular Formula |
C72H96CLN17O16
|
|---|---|
| Molecular Weight |
1491.11
|
| Exact Mass |
1489.69
|
| CAS # |
145672-81-7
|
| Related CAS # |
Cetrorelix; 120287-85-6; Cetrorelix diacetate; 130143-01-0
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| PubChem CID |
25078429
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| Appearance |
White to off-white solid powder
|
| LogP |
6.023
|
| Hydrogen Bond Donor Count |
17
|
| Hydrogen Bond Acceptor Count |
18
|
| Rotatable Bond Count |
38
|
| Heavy Atom Count |
106
|
| Complexity |
2870
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
C[C@H](C(=O)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCNC(=O)N)NC(=O)[C@H](CC2=CC=C(C=C2)O)NC(=O)[C@H](CO)NC(=O)[C@@H](CC3=CN=CC=C3)NC(=O)[C@@H](CC4=CC=C(C=C4)Cl)NC(=O)[C@@H](CC5=CC6=CC=CC=C6C=C5)NC(=O)C.CC(=O)O
|
| InChi Key |
KFEFLCOCAHJBEA-ANRVCLKPSA-N
|
| InChi Code |
InChI=1S/C70H92ClN17O14.C2H4O2/c1-39(2)31-52(61(94)82-51(15-9-28-77-69(73)74)68(101)88-30-10-16-58(88)67(100)79-40(3)59(72)92)83-60(93)50(14-8-29-78-70(75)102)81-63(96)54(34-43-20-25-49(91)26-21-43)86-66(99)57(38-89)87-65(98)56(36-45-11-7-27-76-37-45)85-64(97)55(33-42-18-23-48(71)24-19-42)84-62(95)53(80-41(4)90)35-44-17-22-46-12-5-6-13-47(46)32-44;1-2(3)4/h5-7,11-13,17-27,32,37,39-40,50-58,89,91H,8-10,14-16,28-31,33-36,38H2,1-4H3,(H2,72,92)(H,79,100)(H,80,90)(H,81,96)(H,82,94)(H,83,93)(H,84,95)(H,85,97)(H,86,99)(H,87,98)(H4,73,74,77)(H3,75,78,102);1H3,(H,3,4)/t40-,50-,51+,52+,53-,54+,55-,56-,57+,58+;/m1./s1
|
| Chemical Name |
(2S)-1-[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-acetamido-3-naphthalen-2-ylpropanoyl]amino]-3-(4-chlorophenyl)propanoyl]amino]-3-pyridin-3-ylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-5-(carbamoylamino)pentanoyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-N-[(2R)-1-amino-1-oxopropan-2-yl]pyrrolidine-2-carboxamide;acetic acid
|
| Synonyms |
SB 075 acetate; NS-75-A; SB075 acetate; NS-75 A; Cetrorelix acetate; Cetrorelix; Cetrotide; D 20761; D-20761; D20761; NS-75A; NS 75A; SB-075 acetate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~33.5 mM)
H2O: ~2 mg/mL (~1.3 mM) |
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.6706 mL | 3.3532 mL | 6.7064 mL | |
| 5 mM | 0.1341 mL | 0.6706 mL | 1.3413 mL | |
| 10 mM | 0.0671 mL | 0.3353 mL | 0.6706 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05972902 | Recruiting | Drug: Dydrogesterone Drug: Cetrorelix acetate Drug: Triptorelin |
IVF | Beni-Suef University | July 15, 2023 | Phase 3 |
| NCT03680053 | Recruiting | Drug: Duphaston Drug: Cetrorelix |
Infertility ART |
ShangHai Ji Ai Genetics & IVF Institute |
April 10, 2020 | Not Applicable |
| NCT06023602 | Not yet recruiting | Drug: Generic cetrorelix acetate Drug: Reference cetrorelix acetate |
Infertility | Northwest Women's and Children's Hospital, Xi'an, Shaanxi |
December 1, 2023 | Not Applicable |
| NCT05738382 | Not yet recruiting | Drug: BG2109 Drug: Cetrorelix |
Assisted Reproductive Technology Controlled Ovarian Hyperstimulation |
Bio Genuine (Shanghai) Biotech Co., Ltd. |
August 2023 | Phase 2 |
| NCT05951400 | Not yet recruiting | Drug: Dydrogesterone Tablets Drug: Cetrorelix |
IVF PCO |
Beni-Suef University | August 20, 2023 | Phase 2 Phase 3 |
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