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Rogaratinib FGFR inhibitor

Name: Rogaratinib
Brand: Selleck Chemicals
SKU: S8547
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S8547

Rogaratinib(BAY-1163877) is a highly potent and selective small molecule inhibitor of pan‐FGFR kinase activity, which specifically inhibits FGFR1, 2, 3 and 4 with an IC50 values of 1.8 nM, <1 nM, 9.2 nM and 1.2 nM respectively. It demonstrates robust efficacy in cancers with altered FGFR mRNA expression.

Chemical Structure

Molecular Weight: 466.56

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Quality Control

Batch: Purity: 96.55%

96.55

Related Targets	EGFR VEGFR PDGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Other FGFR Inhibitors	PD173074 AZD4547 (Fexagratinib) BLU9931 Futibatinib (TAS-120) LY2874455 H3B-6527 PD-166866 Fisogatinib (BLU-554) Zoligratinib (Debio-1347) SSR128129E

Solubility

In vitro
Batch:

DMSO : 8 mg/mL (17.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/ml (1.71mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.150mg/ml (0.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	466.56	Formula	C₂₃H₂₆N₆O₃S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1443530-05-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BAY-1163877			SMILES	CC1=CC2=C(C(=C1)OC)SC(=C2)C3=C4C(=NC=NN4C(=C3COC)CN5CCNC(=O)C5)N

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	FGFR2 <1 nM FGFR4 1.2 nM FGFR1 1.8 nM FGFR3 9.2 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/30807645/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-31)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04595747	ACTIVE_NOT_RECRUITING	Locally Advanced Gastrointestinal Stromal Tumor; Locally Advanced Sarcoma; Metastatic Gastrointestinal Stromal Tumor; Metastatic Sarcoma; Stage III Gastric and Omental Gastrointestinal Stromal Tumor AJCC v8; Stage III Small Intestinal, Esophageal, Colorectal, Mesenteric, and Peritoneal Gastrointestinal Stromal Tumor AJCC v8; Stage IV Gastric and Omental Gastrointestinal Stromal Tumor AJCC v8; Stage IV Small Intestinal, Esophageal, Colorectal, Mesenteric, and Peritoneal Gastrointestinal Stromal Tumor AJCC v8	National Cancer Institute (NCI)	2021-05-03	PHASE2
NCT04483505	COMPLETED	Breast Cancer Metastatic; Hormone Receptor Positive Malignant Neoplasm of Breast	Fundacion CRIS de Investigación para Vencer el Cáncer	2020-11-25	PHASE1
NCT03762122	TERMINATED	Squamous-cell Non-small Cell Lung Cancer	Swiss Cancer Institute	2019-07-25	PHASE2
NCT03473756	COMPLETED	Urothelial Carcinoma	Bayer	2018-05-15	PHASE1
NCT04125693	COMPLETED	Cancer	Bayer	2019-10-30	PHASE2
NCT03517956	COMPLETED	Advanced or Metastatic Solid Tumor	Bayer	2018-07-25	PHASE1

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