Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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ln Vitro |
Rintodestrant (G1T48), like pure antiestrogen fulvestrant, is a strong and effective inhibitor of estrogen-mediated transcription and proliferation in ER-positive breast cancer cells[1]. Only ER-positive breast cancer cells are preferentially inhibited in their proliferation by rindodestrant (G1T48)[1].
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ln Vivo |
In endocrine-resistant breast cancer models, rimodestrant (G1T48, 30 or 100 mg/kg) blocks estrogen signaling[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: MCF7 cells. Tested Concentrations: 1 pM-1 μM. Incubation Duration: 18 h. Experimental Results: Downregulates the estrogen receptor in breast cancer cells. Dramatically inhibited estrogen-mediated growth of MCF7 cells demonstrating approximately threefold higher potency when compared to Fulvestrant. Does not impact apoptosis in MCF7 breast cancer cells. |
Animal Protocol |
Animal/Disease Models: MCF7 xenograft tumors[1] ].
Doses: 30 or 100 mg/kg. Route of Administration: PO daily for 28 days. Experimental Results: Demonstrated dose-dependent inhibition of TamR tumor growth. |
References |
[1]. Kaitlyn J Andreano, et al. G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Res Treat. 2020 Apr;180(3):635-646.
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Molecular Formula |
C26H19FO5S
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Molecular Weight |
462.49
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CAS # |
2088518-51-6
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Related CAS # |
2088518-51-6;
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S1C2C=C(C=CC=2C(=C1C(C1C(C)=CC(=CC=1C)F)=O)OC1C=CC(/C=C/C(=O)O)=CC=1)O
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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 |
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 (108.11 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1622 mL | 10.8110 mL | 21.6221 mL | |
5 mM | 0.4324 mL | 2.1622 mL | 4.3244 mL | |
10 mM | 0.2162 mL | 1.0811 mL | 2.1622 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.