| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Rogaratinib (formerly also known as BAY1163877; BAY-1163877) is a novel, orally available, potent and selective inhibitor of aberrant fibroblast growth factor receptor (FGFR) with anticancer activity. In lung cancer (LC), aberrant activation or expression of the fibroblast growth factor receptor (FGFR) is frequently observed. The receptor tyrosine kinases FGFR-1, -2, and -3 are inhibited by rogaratinib. These kinases are upregulated in different types of tumor cells and may play a role in the differentiation, proliferation, angiogenesis, and survival of tumor cells.
| Targets |
FGFR1; FGFR2; FGFR3; FGFR4
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|---|---|
| ln Vitro |
The FGFR1-amplified lung cancer (LC) cell lines H1581 and DMS114, which have GI50 values ranging from 36 to 244 nM, exhibit extreme sensitivity to rogaratinib (BAY1163877) out of the 24 cell lines. When H1581P cells are treated with rogaratinib, their ability to form colonies is significantly reduced, but H1581AR and BR cell colonies are not affected. Rogaratinib resistance is markedly increased in MTT assays by ectopic expression of Met. Metabolic overexpression triggers the activation of AKT and downstream extracellular signal-regulated kinase 1/2 (ERK1/2), which is irreversible upon treatment with rogaratinib[1].
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| Cell Assay |
On 96-well plates, cells are seeded at 37°C (3000 cells/well). Following a night of incubation, the cells receive a 72-hour Rogaratinib treatment. After that, each well is filled with MTT reagent (3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide), which is then incubated for four hours at 37°C. Each well is filled with MTT solubilization solution/stop mix, combined, and the plates are then incubated at 37°C for the entire night. The data are shown graphically once the absorbance at 570 nm has been measured[1].
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| References |
| Molecular Formula |
C23H26N6O3S
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|---|---|
| Molecular Weight |
466.555943012238
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| Exact Mass |
466.18
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| Elemental Analysis |
C, 59.21; H, 5.62; N, 18.01; O, 10.29; S, 6.87
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| CAS # |
1443530-05-9
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| Related CAS # |
1443530-05-9
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| Appearance |
Solid powder
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| SMILES |
CC1=CC2=C(C(=C1)OC)SC(=C2)C3=C4C(=NC=NN4C(=C3COC)CN5CCNC(=O)C5)N
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| InChi Key |
HNLRRJSKGXOYNO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H26N6O3S/c1-13-6-14-8-18(33-22(14)17(7-13)32-3)20-15(11-31-2)16(9-28-5-4-25-19(30)10-28)29-21(20)23(24)26-12-27-29/h6-8,12H,4-5,9-11H2,1-3H3,(H,25,30)(H2,24,26,27)
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| Chemical Name |
4-[[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methyl-1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-7-yl]methyl]piperazin-2-one
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| Synonyms |
Rogaratinib; BAY1163877; BAY-1163877; BAY 1163877
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~5 mg/mL (~10.7 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.56 mg/mL (1.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.56 mg/mL (1.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.6 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.56 mg/mL (1.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03473756 | Active Recruiting |
Drug: Rogaratinib (BAY1163877) Drug: Atezolizumab |
Urothelial Carcinoma | Bayer | May 15, 2018 | Phase 1 |
| NCT04595747 | Active Recruiting |
Drug: Rogaratinib Procedure: Biopsy |
Locally Advanced Sarcoma Metastatic Sarcoma |
National Cancer Institute (NCI) |
May 3, 2021 | Phase 2 |
| NCT03788603 | Completed | Drug: Rogaratinib (BAY1163877) |
Neoplasms | Bayer | January 7, 2019 | Phase 1 |
| NCT03484585 | Completed | Drug: Rogaratinib (BAY1163877) |
Clinical Trial, Phase I Pharmacokinetics |
Bayer | April 6, 2018 | Phase 1 |
| NCT03410693 | Completed | Drug: Rogaratinib (BAY1163877) |
Carcinoma, Transitional Cell | Bayer | May 31, 2018 | Phase 2 Phase 3 |
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