2. Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. Estrogen Receptor/ERR CDK
  4. Rintodestrant

Rintodestrant  (Synonyms: G1T48)

Cat. No.: HY-137449 Purity: 99.79%
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Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor.

For research use only. We do not sell to patients.

Rintodestrant Chemical Structure

Rintodestrant Chemical Structure

CAS No. : 2088518-51-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 550 In-stock
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Solid
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1650 In-stock
50 mg USD 2600 In-stock
100 mg USD 4200 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Rintodestrant Related Antibodies

Top Publications Citing Use of Products

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

View All CDK Isoform Specific Products:

View All Isoforms
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Rintodestrant (G1T48) is an orally active, non-steroidal and selective estrogen receptor degrader. Rintodestrant (G1T48) is also a CDK4/6 inhibitor[1].

In Vitro

Rintodestrant (G1T48) is a potent and efficacious inhibitor of estrogen-mediated transcription and proliferation in ER-positive breast cancer cells, similar to the pure antiestrogen fulvestrant[1].
Rintodestrant (G1T48) selectively inhibits the growth of ER-positive, but not ER-negative, breast cancer cells[1].

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

Rintodestrant Related Antibodies

Cell Viability Assay[1]

Cell Line: MCF7 cells.
Concentration: 1 pM-1 μM.
Incubation Time: 18 h.
Result: Downregulates the estrogen receptor in breast cancer cells.
Significantly 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.
In Vivo

Rintodestrant (G1T48, 30 or 100 mg/kg) inhibits estrogen signaling in endocrine-resistant breast cancer models[1].

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

Animal Model: MCF7 xenograft tumors[1].
Dosage: 30 or 100 mg/kg.
Administration: P.O. daily for 28 days.
Result: Demonstrated dose-dependent inhibition of TamR tumor growth.
Clinical Trial
Molecular Weight

462.49

Formula

C26H19FO5S
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=C(C(C(C)=CC(F)=C1)=C1C)C(SC2=C3)=C(C2=CC=C3O)OC(C=C4)=CC=C4/C=C/C(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (108.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.79%

SDS (251 KB)

COA (256 KB) HNMR (307 KB) LCMS (262 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1622 mL 10.8110 mL 21.6221 mL 54.0552 mL
5 mM 0.4324 mL 2.1622 mL 4.3244 mL 10.8110 mL
10 mM 0.2162 mL 1.0811 mL 2.1622 mL 5.4055 mL
15 mM 0.1441 mL 0.7207 mL 1.4415 mL 3.6037 mL
20 mM 0.1081 mL 0.5406 mL 1.0811 mL 2.7028 mL
25 mM 0.0865 mL 0.4324 mL 0.8649 mL 2.1622 mL
30 mM 0.0721 mL 0.3604 mL 0.7207 mL 1.8018 mL
40 mM 0.0541 mL 0.2703 mL 0.5406 mL 1.3514 mL
50 mM 0.0432 mL 0.2162 mL 0.4324 mL 1.0811 mL
60 mM 0.0360 mL 0.1802 mL 0.3604 mL 0.9009 mL
80 mM 0.0270 mL 0.1351 mL 0.2703 mL 0.6757 mL
100 mM 0.0216 mL 0.1081 mL 0.2162 mL 0.5406 mL
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Rintodestrant Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rintodestrant2088518-51-6G1T48Estrogen Receptor/ERRCDKCyclin dependent kinasebreastcancerCDK4CDK6fulvestrantInhibitorinhibitorinhibit

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