1443530-05-9
1443530-05-9
Chemical Structure
Rogaratinib
Synonym(s): BAY1163877
- CAS No.: 1443530-05-9
- Formula:C23H26N6O3S
- Molecular Weight:466.56
IUPAC Name: 4-((4-amino-5-(7-methoxy-5-methylbenzo[b]thiophen-2-yl)-6-(methoxymethyl)pyrrolo[2,1-f][1,2,4]triazin-7-yl)methyl)piperazin-2-one
InChIKey: HNLRRJSKGXOYNO-UHFFFAOYSA-N
SMILES: O=C1NCCN(CC2=C(COC)C(C3=CC4=CC(C)=CC(OC)=C4S3)=C5C(N)=NC=NN52)C1
Biological Activity: 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[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Rogaratinib | 99.86% | 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. | ||||||||||||||||||||
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PI3Kδ-IN-1 (Standard) | ≥98% | PI3Kδ-IN-1 (Standard) is the analytical standard of PI3Kδ-IN-1 (HY-101921). This product is intended for research and analytical applications. PI3Kδ-IN-1 is a potent, selective, and efficacious PI3Kδ inhibitor with an IC50 of 1.7 nM. | ||||||||||||||||||||
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MLK-IN-1 | 99.07% | MLK-IN-1 is a potent, brain penetrant and specific mixed lineage kinase 3 (MLK-3) inhibitor, compound 68, extracted from patent US20140256733A1. | ||||||||||||||||||||
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SRT 1460 | 98.16% | SRT 1460, a potent Sirtuin-1 (SIRT1) activator with an EC1.5 value of 2.9 μM, shows good selectivity for activation of SIRT1 versus SIRT2 and SIRT3 (EC1.5>300 μM), and is more potent than Resveratrol and the closest sirtuin homologues. | ||||||||||||||||||||
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Afimetoran | 99.37% | Afimetoran (BMS-986256) is an orally active, selective, and highly bioavailable TLR7/8 antagonist. Afimetoran (BMS-986256) can inhibit TLR7/8 activation of the NF-κB pathway and reverse TLR7 mediated resistance to steroid induced apoptosis in plasma cell like dendritic cells (pDCs). Afimetoran (BMS-986256) can be used for research on inflammation and autoimmune diseases (systemic lupus erythematosus). | ||||||||||||||||||||
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EGFR-IN-35 | EGFR-IN-35 is a potent inhibitor of EGFR. EGFR-IN-35 is an anti-tumor agent with low toxic side effects. EGFR-IN-35 is an acrylamide derivative compound. Overexpression and mutation of the epidermal growth factor receptor (EGFR) has been clearly demonstrated to lead to uncontrollable cell growth and is associated with the progression of most cancer diseases, especially NSCLC. EGFR-IN-35 has the potential for the research of diseases associated with EGFR mutations (extracted from patent WO2021185348A1, compound 11). | |||||||||||||||||||||
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EGFR-IN-36 | EGFR-IN-36 is a potent EGFR inhibitor with IC50s of 19.09 nM, 120.01 nM, 2.35 nM for EGFR (WT), HER2 (WT), HER2 (A775_G776insYVMA), respectively. EGFR-IN-36 has potential for wild and/or mutant EGFR and/or HER2 kinase mediated tumors research. | |||||||||||||||||||||
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(S)-HH2853 | (S)-HH2853 (compound 200), a PYRIDINO five membered aromatic ring compound, is a potent EZH1/2 dual inhibitor with an IC50 of <100 nM for EZH2_Y641F. (S)-HH2853 has the potential to be used in the research of anti-tumor or autoimmune diseases. | |||||||||||||||||||||
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(R)-HH2853 | (R)-HH2853 is a mutant EZH2 inhibitor with an IC50 of <100 nM for EZH2-Y641F. (R)-HH2853 can be used for cancer and autoimmune diseases (WO2018045971A1; compound 201). | |||||||||||||||||||||
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RSV L-protein-IN-5 | RSV L-protein-IN-5 (compound E) is a potent inhibitor of Respiratory syncytial virus (RSV) (EC50=0.1 μM). RSV L-protein-IN-5 inhibits Polymerase (IC50=0.66 μM)，and blocks RSV mRNA synthesis by inhibiting guanylation of viral transcripts. RSV L-protein-IN-5 shows moderate cytotoxicity (CC50=10.7 μM，HEp-2)，also exhibits activity and lowers virus titers in mouse models of RSV infection. | |||||||||||||||||||||
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EOC317 | 98.01% | EOC317 (ACTB-1003) is an oral kinase inhibitor with IC50s of 6, 2 and 4 nM for FGFR1, VEGFR2 and Tie-2. | ||||||||||||||||||||
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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]
