Rogaratinib (BAY1163877)

Rogaratinib (BAY1163877) - Names and Identifiers

Name	BAY-1163877
Synonyms	BAY-1163877 Rogaratinib Rogaratinib (BAY1163877) 2-Piperazinone, 4-[[4-amino-6-(methoxymethyl)-5-(7-methoxy-5-methylbenzo[b]thien-2-yl)pyrrolo[2,1-f][1,2,4]triazin-7-yl]methyl]- 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
CAS	1443530-05-9

Rogaratinib (BAY1163877) - Physico-chemical Properties

Molecular Formula	C23H26N6O3S
Molar Mass	466.56
Density	1.48±0.1 g/cm3(Predicted)
Solubility	DMSO :2 mg/mL ( Need ultrasonic)
pKa	15.49±0.20(Predicted)
Storage Condition	-20°C
Use	Rogaratinib, also known as BAY-1163877, is an aberrant fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity. FGFRs are a family of receptor tyrosine kinases, which may be upregulated in various tumor cell types and may be involved in tumor cell differentiation and proliferation, tumor angiogenesis, and tumor cell survival.
Target	FGFR

Rogaratinib (BAY1163877) - Upstream Downstream Industry

Raw Materials

6-(methoxymethyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine
ETHYL 4-AMINOPYRROLO[2,1-F][1,2,4]TRIAZINE-6-CARBOXYLATE
Pyrrolo[2,1-f][1,2,4]triazine-6-methanol, 4-amino-
Benzenethiol, 2-methoxy-4-methyl-
7-Methoxy-5-Methylbenzo[b]thiophene
(7-Methoxy-5-Methylbenzo[b]thiophen-2-yl)boronic acid
2-Piperazinone
2-methoxy-p-toluidine
(2,2-diethoxyethyl)(2-methoxy-4-methylphenyl)sulfane
2-METHOXY-4-METHYLBENZENESULFONYL CHLORIDE
4-AMinopyrrolo[1,2-f][1,2,4]triazine-6-carbonitrile
5-METHYL-2-NITROANISOLE
Formaldehyde

Rogaratinib (BAY1163877) - Reference

Reference

1. Sylvia Grünewald , Oliver Politz , Sebastian Bender,et al.Rogaratinib: A potent and selective pan-FGFR inhibitor with broad antitumor activity in FGFR-overexpressing preclinical cancer models.Int J Cancer. 2019 Sep 1;145(5):1346-1357.2. 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.