Erdafitinib (JNJ-42756493) - Moligand™, 10mM in DMSO , Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fibroblast growth factor receptor 2;Inhibitor of fibroblast growth factor receptor 3;Inhibitor of fibroblast growth factor receptor 4;Inhi, Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fibroblast growth factor receptor 2;Inhibitor of fibroblast growth factor receptor 3;Inhibitor of fibroblast growth factor receptor 4;Inhibitor of kinase insert domain receptor

CAS: 1346242-81-6 Cat. No.: E409267 Summenformel: C₂₅H₃₀N₆O₂ Molekulargewicht: 446.54 EG-Nummer: 807-395-6

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

1,​2-​Ethanediamine, N1-​(3,​5-​dimethoxyphenyl)​-​N2-​(1-​methylethyl)​-​N1-​[3-​(1-​methyl-​1H-​pyrazol-​4-​yl)​-​6-​quinoxalinyl]​-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

Information

Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, panfibroblast growth factor receptor (FGFR)inhibitor with potential antineoplastic activity. Erdafitinib also binds toRET (c-RET),CSF-1R,PDGFR-α/PDGFR-β,FLT4,Kit (c-Kit)andVEGFR-2an
In vitro

JNJ-42756493 is a potent, oral pan-FGFR tyrosine kinase inhibitor with half-maximal inhibitory concentration values in the low nanomolar range for all members of the FGFR family (FGFR1 to FGFR4), with minimal activity on vascular endothelial growth factor receptor (VEGFR) kinases compared with FGFR kinases (approximately 20-fold potency difference). In vitro, the proliferation of cells treated with JNJ-42756493 is decreased, associated with increased apoptotic death and decreased cell survival.

In vivo

In vivo, growth of NCI-H716 tumors is delayed by 5 days by drug treatment alone, although when drug delivery is stopped the relative tumor volume increased compared to control. JNJ-42756493 shows favorable drug like properties and displays a high distribution to lung, liver and kidney tissue. JNJ-42756493 is well tolerated at efficacious doses and results in potent dose-dependent antitumor activity accompanied by pharmacodynamic modulation of tumor FGFR and downstream pathway components.
Cell Data

cell lines：HeLa, MCF7, HCT-116, U2OS, A2780, K562, SF-539, SF-268, Ovcar8, SW480, COLO205, HCT-15, Jurkat, PC3, and NHDF

Concentrations：--

Incubation Time：72 h

Powder Purity:≥99%

Specifications

Synonyme

1,​2-​Ethanediamine, N1-​(3,​5-​dimethoxyphenyl)​-​N2-​(1-​methylethyl)​-​N1-​[3-​(1-​methyl-​1H-​pyrazol-​4-​yl)​-​6-​quinoxalinyl]​-

Spezifikationen & Reinheit

Moligand™, 10mM in DMSO

Biochemische und physiologische Mechanismen

Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and

Storage

Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Note

Moligand™

Aktionsart

INHIBITOR

Mechanismus der Wirkung

Inhibitor of fibroblast growth factor receptor 1;Inhibitor of fibroblast growth factor receptor 2;Inhibitor of fibroblast growth factor receptor 3;Inhibitor of fibroblast growth factor receptor 4;Inhibitor of kinase insert domain receptor

Produkteigenschaften

• ALogP: 3.943
• hba_count: 5
• HBD-Zahl: 1
• Rotationsfähige Bindung: 9

Namen und Kennungen

• Isomere SMILES: CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC
• Alternative CAS-Nummer: 1346242-81-6
• MeSH-Eintrag: Balversa;erdafitinib;JNJ-42756493
• Molekulargewicht: 446.54
• Reaxy-Rn: 21971528
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=21971528&ln=

Zugehörige Ziele (menschlich)

FGFR1 Tclin Fibroblast growth factor receptor 1 (5 Activities)

Discover Target: FGFR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR2 Tclin Fibroblast growth factor receptor 2 (5 Activities)

Discover Target: FGFR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR4 Tclin Fibroblast growth factor receptor 4 (6 Activities)

Discover Target: FGFR4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 (9 Activities)

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KDR Tclin Vascular endothelial growth factor receptor 2 (1 Activities)

Discover Target: KDR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemische und physikalische Eigenschaften

• Löslichkeit: Solubility (25°C) In vitro DMSO: 66 mg/mL (201.33 mM); Ethanol: 66 mg/mL (201.33 mM); Water: Insoluble
• DMSO (mg/ml) Maximale Löslichkeit: 89
• DMSO (mM) Maximale Löslichkeit: 199.3102522
• Wasser (mg/ml) Maximale Löslichkeit: ＜1
• Schmelzpunkt (°C): 136-140°C