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Rogaratinib

Catalog No. T16781 CAS 1443530-05-9

Synonyms: BAY1163877

Rogaratinib is an aberrant inhibitor of fibroblast growth factor receptor (FGFR). Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity.

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Rogaratinib, CAS 1443530-05-9

Pack Size	Availability	Price/USD	Quantity
1 mg	5 days	$ 79.00

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

Rogaratinib is an aberrant inhibitor of fibroblast growth factor receptor (FGFR). Rogaratinib is as an orally available, selective and potent inhibitor of FGFR-1, -2 and -3 kinase activity.

In vitro

A novel pan-FGFR inhibitor, rogaratinib, in biochemical, cellular and in vivo efficacy studies in a variety of preclinical cancer models.?In vitro kinase activity assays demonstrate that rogaratinib potently and selectively inhibits the activity of FGFRs 1, 2, 3 and 4.?In line with this, rogaratinib reduced proliferation in FGFR-addicted cancer cell lines of various cancer types including lung, breast, colon and bladder cancer.?FGFR and ERK phosphorylation interruption by rogaratinib treatment in several FGFR-amplified cell lines suggests that the anti-proliferative effects are mediated by FGFR/ERK pathway inhibition[1].

Synonyms	BAY1163877
Molecular Weight	466.56
Formula	C23H26N6O3S
CAS No.	1443530-05-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

Solubility Information

DMSO: 5.5 mg/mL (11.78 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

Related Products

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CP-547632 FIIN-1 FIIN-4 Infigratinib phosphate S49076 HCl CP-547632 hydrochloride SSR128129E free acid FGFR4-IN-4

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Rogaratinib 1443530-05-9 Angiogenesis Tyrosine Kinase/Adaptors FGFR inhibit BAY 1163877 Fibroblast growth factor receptor BAY-1163877 BAY1163877 Inhibitor inhibitor

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