Rogaratinib
Based on 7 publication(s) in Google Scholar
Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib inhibits FGFRs with IC50s of 11.2 nM (FGFR1), <1 nM (FGFR2), 18.5 nM (FGFR3), 127 nM (VEGFR3/FLT4), 201 nM (FGFR4), respectively.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.86%
- CAS No.: 1443530-05-9
- Formule: C23H26N6O3S
- Masse moléculaire:466.56
-
Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
-
HY-18708
ErdafitinibFGFR Inhibitor -
HY-109099
PemigatinibFGFR Inhibitor -
HY-13330
FexagratinibFGFR Inhibitor -
HY-19981
Derazantinib -
HY-100818
FutibatinibFGFR Inhibitor -
HY-13311
InfigratinibFGFR Inhibitor -
HY-19957
Zoligratinib -
HY-13304
LY2874455FGFR Inhibitor -
HY-100491
H3B-6527FGFR4 Inhibitor -
HY-101768
PRN1371FGFR Inhibitor -
HY-100492
FisogatinibFGFR4 Inhibitor -
HY-101568
RoblitinibFGFR4 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Rogaratinib
More- Nat Med. 2026 May 26.
- NPJ Precis Oncol. 2025 Nov 7;9(1):343. [Abstract]
- ACS Appl Mater Interfaces. 2021 May 5;13(17):19768-19777. [Abstract]
- Mol Syst Biol. 2024 Jan;20(1):28-55. [Abstract]
- Anticancer Drugs. 2023 Oct 1;34(9):1035-1045. [Abstract]
- Patent. US11768205B2.
- IOP Conf Ser Mater Sci Eng. 562 (2019) 012128.
Customer Validation & Images
-
WB
Activité biologique
Description
IC50 & Target
[1]|
FGFR1 |
FGFR2 |
FGFR3 |
FGFR4 |
In Vitro
Of the 24 cell lines, 2 FGFR1-amplified lung cancer (LC) cell lines, H1581 and DMS114, show extreme sensitivity to Rogaratinib (BAY1163877) (GI50 values ranging from 36 to 244 nM). Treatment with Rogaratinib results in a significant decrease in colonies formed by H1581P cells, but not by H1581AR and BR cells. Ectopic expression of Met significantly induces resistance to Rogaratinib in MTT assays. Met overexpression induces activation of downstream extracellular signal-regulated kinase 1/2 (ERK1/2) and AKT, which cannot be abrogated by Rogaratinib treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1443530-05-9
-
Appearance Solid
-
Masse moléculaire 466.56
-
Formule C23H26N6O3S
-
Color White to light yellow
-
SMILES
O=C1NCCN(CC2=C(COC)C(C3=CC4=CC(C)=CC(OC)=C4S3)=C5C(N)=NC=NN52)C1
-
Synonyms
BAY1163877
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
-
Journal Impact Factor
-
Most Recent
-
-
NPJ Precis Oncol
Co-clinical trial targeting ER, FGFR and CDK4/6 in resistant hormone-positive breast cancer with FGFR alterations. [Abstract]2025 Nov 7;9(1):343. PMID: 41203797 -
ACS Appl Mater Interfaces
2021 May 5;13(17):19768-19777. PMID: 33877794 -
Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929 -
Anticancer Drugs
Derazantinib, a fibroblast growth factor receptor inhibitor, inhibits colony-stimulating factor receptor-1 in macrophages and tumor cells and in combination with a murine programmed cell death ligand-1-antibody activates the immune environment of murine syngeneic tumor models. [Abstract]2023 Oct 1;34(9):1035-1045. PMID: 36729099 -
-
Rogaratinib purchased from MedChemExpress. Usage Cited in: IOP Conf Ser Mater Sci Eng. 562 (2019) 012128.
Effects of BAY1163877 on the Expression of p-FGFR1/FGFR1 and p-STAT3/STAT3 Protein in Breast Cancer Cell Lines MDA-MB-231 and MCF-7 are showed.
Solvant et solubilité
In Vitro:
DMSO : 5 mg/mL (10.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.56 mg/mL (1.20 mM); Clear solution
This protocol yields a clear solution of ≥ 0.56 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.6 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.56 mg/mL (1.20 mM); Clear solution
This protocol yields a clear solution of ≥ 0.56 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.6 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
-
Fiche technique (283 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1433 mL | 10.7167 mL | 21.4335 mL | 53.5837 mL |
| 5 mM | 0.4287 mL | 2.1433 mL | 4.2867 mL | 10.7167 mL | |
| 10 mM | 0.2143 mL | 1.0717 mL | 2.1433 mL | 5.3584 mL |
Rogaratinib Related Classifications
HY-100019 Related Classifications
Powered by Bioz