Rintodestrant

Name: Rintodestrant
Brand: TargetMol
SKU: T39499
Rating: 4.5 (1 reviews)

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Catalog No. T39499Cas No. 2088518-51-6

Alias G1T48

Rintodestrant (G1T48) is an orally active, non-steroidal, selective estrogen receptor degrader (SERD) and CDK4/6 inhibitor.

Rintodestrant

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Catalog No. T39499Alias G1T48Cas No. 2088518-51-6

Rintodestrant (G1T48) is an orally active, non-steroidal, selective estrogen receptor degrader (SERD) and CDK4/6 inhibitor.

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Product Introduction

Bioactivity

Description	Rintodestrant (G1T48) is an orally active, non-steroidal, selective estrogen receptor degrader (SERD) and CDK4/6 inhibitor.
In vitro	Rintodestrant (G1T48) serves as a potent and effective inhibitor, targeting estrogen-mediated transcription and proliferation specifically in ER-positive breast cancer cells, mirroring the efficacy of the pure antiestrogen agent fulvestrant. Its activity is exclusive to ER-positive breast cancer cells, showing no effect on ER-negative cell types. In a Cell Viability Assay utilizing MCF7 cells at concentrations ranging from 1 pM to 1 μM over an incubation period of 18 hours, Rintodestrant demonstrated a significant downregulation of the estrogen receptor, markedly inhibiting estrogen-stimulated growth in these cells with a potency approximately threefold greater than that of Fulvestrant. Notably, this inhibition does not influence apoptosis within MCF7 breast cancer cells.
In vivo	Rintodestrant (G1T48, 30 or 100 mg/kg) effectively suppresses estrogen signaling in models of endocrine-resistant breast cancer, specifically in MCF7 xenograft tumors[1]. Administered orally at doses of 30 or 100 mg/kg daily for 28 days, it exhibits a dose-dependent reduction in TamR tumor growth.
Synonyms	G1T48

Chemical Properties

Molecular Weight	462.49
Formula	C₂₆H₁₉FO₅S
Cas No.	2088518-51-6
Smiles	Cc1cc(F)cc(C)c1C(=O)c1sc2cc(O)ccc2c1Oc1ccc(\C=C\C(O)=O)cc1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc