Rogaratinib (Synonyms: BAY1163877)

Name: Rogaratinib
Brand: MedChemExpress
SKU: HY-100019
Rating: 5.0 (6 reviews)

Cat. No.: HY-100019 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

Rogaratinib Chemical Structure

CAS No. : 1443530-05-9

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 216	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 216	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 210	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 380	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2250	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 6 publication(s) in Google Scholar

5 Publications Citing Use of MCE Rogaratinib

: 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.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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.

Clinical Trial

Molecular Weight

466.56

Formula

C₂₃H₂₆N₆O₃S

CAS No.

1443530-05-9

Appearance

Solid

Color

White to light yellow

SMILES

O=C1NCCN(CC2=C(COC)C(C3=CC4=CC(C)=CC(OC)=C4S3)=C5C(N)=NC=NN52)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1433 mL	10.7167 mL	21.4335 mL
5 mM	0.4287 mL	2.1433 mL	4.2867 mL
10 mM	0.2143 mL	1.0717 mL	2.1433 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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.56 mg/mL (1.20 mM); Clear solution

This protocol yields a clear solution of ≥ 0.56 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.6 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.86%

Select Batch:

Data Sheet (283 KB) SDS (393 KB)

COA (261 KB) HNMR (251 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Heroult M, et al. Preclinical profile of BAY 1163877-a selective pan-FGFR inhibitor in phase 1 clinical trial[J]. Cancer Res, 2014, 74(suppl 19): 1739a.

[2]. Kim SM, et al. Activation of the Met kinase confers acquired drug resistance in FGFR-targeted lung cancer therapy. Oncogenesis. 2016 Jul 18;5(7):e241. [Content Brief]

Cell Assay
^[1]

Cells (3000 cells/well) are seeded on 96-well plates at 37°C. After overnight incubation, the cells are treated with Rogaratinib for 72 h. Then, MTT reagent [3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide] is added to each well and incubated for 4 h at 37°C. MTT solubilization solution/stop mix is added to each well, mixed, and the plates are incubated overnight at 37°C. After measuring the absorbance at 570 nm, the data are graphically displayed^[1].

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

References

[1]. Heroult M, et al. Preclinical profile of BAY 1163877-a selective pan-FGFR inhibitor in phase 1 clinical trial[J]. Cancer Res, 2014, 74(suppl 19): 1739a.

[2]. Kim SM, et al. Activation of the Met kinase confers acquired drug resistance in FGFR-targeted lung cancer therapy. Oncogenesis. 2016 Jul 18;5(7):e241. [Content Brief]

Complete Stock Solution Preparation Table

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

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:

Rogaratinib1443530-05-9BAY1163877BAY 1163877BAY-1163877FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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Rogaratinib (Synonyms: BAY1163877)

Customer Review

Rogaratinib Related Antibodies

5 Publications Citing Use of MCE Rogaratinib

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All FGFR Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Rogaratinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Rogaratinib Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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