FGFR2-IN-3
CAS No. 2549174-42-5
FGFR2-IN-3( —— )
Catalog No. M35365 CAS No. 2549174-42-5
FGFR2-IN-3 is an orally active selective FGFR2 inhibitor.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 132 | Get Quote |
|
| 5MG | 202 | Get Quote |
|
| 10MG | 297 | Get Quote |
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| 25MG | 610 | Get Quote |
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| 50MG | 908 | Get Quote |
|
| 100MG | 1197 | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
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Product NameFGFR2-IN-3
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NoteResearch use only, not for human use.
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Brief DescriptionFGFR2-IN-3 is an orally active selective FGFR2 inhibitor.
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DescriptionLirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs.
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In VitroApoptosis AnalysisCell Line:FGFR2-amplified gastric cancer cell line SNU-16 Concentration:IC50 (6 nM), IC90 Incubation Time:24 hResult:Induced dose-dependent cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP)-early markers of apoptosis.Apoptosis Analysis Cell Line:FGFR2-amplified gastric cancer cell line SNU-16 Concentration:IC50 (6 nM), IC90 Incubation Time:2 h Result:Demonstrated a dose-dependent reduction of phosphorylation of FGFR2 signaling pathway nodes, including FRS2, AKT, and ERK.
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In VivoAnimal Model:Female BALB/c nude mice with SNU-16 and AN3CA xenografts; female NOD SCID mice with CC13-7 and ICC13-7-FGFR2V564F xenografts Dosage:1, 3, 10, 30 mg/kg Administration:Orally; twice daily; for 15-30 days Result:Exhibited dose-dependent antitumor activity and induced tumor regression in all models.
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Synonyms——
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PathwayAngiogenesis
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TargetFGFR
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RecptorFGFR
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Research Area——
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Indication——
Chemical Information
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CAS Number2549174-42-5
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Formula Weight509.53
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Molecular FormulaC28H24FN7O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 62.5 mg/mL (122.66 mM; Ultrasonic (<60°C)
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SMILESCC(=C)C(=O)Nc1ccc(cc1)-c1c(-c2ccc(Oc3nccc(C)n3)c(F)c2)c2c(N)ncnc2n1C
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Vivek Subbiah, et al. RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations. Cancer Discov. 2023 Sep 6;13(9):2012-2031.?
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