BGJ398 (Infigratinib)
Catalog No.: GC10055Purity:>99.50%Synonyms: Infigratinib, NVP-BGJ398
BGJ398 (Infigratinib) is an oral, ATP-competitive pan-FGFR tyrosine kinase inhibitor (FGFR1: IC50 = 0.9nM; FGFR2: IC50 = 1.4nM; FGFR3: IC50 = 1nM; FGFR4: IC50 = 60nM).
Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.
Cas No.: 872511-34-7
10mM (in 1mL DMSO)In Stock
$40.00
1
5mgIn Stock
$35.00
1
10mgIn Stock
$49.00
1
50mgIn Stock
$101.00
1
100mgIn Stock
$173.00
1
200mgIn Stock
$293.00
1
500mgIn Stock
$606.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $40.00 | In Stock | 1 | |
| 5mg | $35.00 | In Stock | 1 | |
| 10mg | $49.00 | In Stock | 1 | |
| 50mg | $101.00 | In Stock | 1 | |
| 100mg | $173.00 | In Stock | 1 | |
| 200mg | $293.00 | In Stock | 1 | |
| 500mg | $606.00 | In Stock | 1 |
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Zitate (Citations)
1 publicationsPublikationen von Forschern, die dieses Produkt verwendenBeschreibung (Description)
BGJ398 (Infigratinib) is an oral, ATP-competitive pan-FGFR tyrosine kinase inhibitor (FGFR1: IC50 = 0.9nM; FGFR2: IC50 = 1.4nM; FGFR3: IC50 = 1nM; FGFR4: IC50 = 60nM) [1]. BGJ398 targets the fibroblast growth factor receptors FGFR1, FGFR2, FGFR3, and FGFR4, thereby blocking signal transduction mediated by these receptors and inhibiting FGFR-dependent tumor cell proliferation and angiogenesis [2-3]. BGJ398 is primarily used to treat dwarfism in children [4].
In SKOV3ip1 cells, the survival rate of cell in spheroid culture was significantly reduced after BGJ398 (0.3125-5µM; 72h) treatment [5]. In UMUC-14 cells, the combination of paclitaxel and BGJ398 (0-10µM; 72h) can produce a synergistic effect in promoting cell apoptosis [6].
In TMK-1 cells xenograft mice model, treatment with BGJ398 (10mg/kg; po; 20d) significantly inhibited tumor growth [7]. In Snu16R‑derived xenograft mice model, knockdown of BAG3 enhances the anti-tumor effect induced by BGJ398 (30mg/kg; po; 4 weeks) [8].
References:
[1]. Guagnano V, Furet P, Spanka C, et al. Discovery of 3-(2, 6-dichloro-3, 5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase[J]. Journal of medicinal chemistry, 2011, 54(20): 7066-7083.
[2]. Szymczyk J, Sluzalska K D, Materla I, et al. FGF/FGFR-dependent molecular mechanisms underlying anti-cancer drug resistance[J]. Cancers, 2021, 13(22): 5796.
[3]. Agrawal S, Maity S, AlRaawi Z, et al. Targeting drugs against fibroblast growth factor (s)-induced cell signaling[J]. Current drug targets, 2021, 22(2): 214-240.
[4]. Högler W, Ward L M. New developments in the management of achondroplasia[J]. Wiener Medizinische Wochenschrift, 2020, 170(5): 104-111.
[5]. Cha H J, Choi J H, Park I C, et al. Selective FGFR inhibitor BGJ398 inhibits phosphorylation of AKT and STAT3 and induces cytotoxicity in sphere-cultured ovarian cancer cells[J]. International Journal of Oncology, 2017, 50(4): 1279-1288.
[6]. Kim S H, Ryu H, Ock C Y, et al. BGJ398, a pan-FGFR inhibitor, overcomes paclitaxel resistance in urothelial carcinoma with FGFR1 overexpression[J]. International journal of molecular sciences, 2018, 19(10): 3164.
[7]. Schmidt K, Moser C, Hellerbrand C, et al. Targeting fibroblast growth factor receptor (FGFR) with BGJ398 in a gastric cancer model[J]. Anticancer Research, 2015, 35(12): 6655-6665.
[8]. Li K, Deng X, Feng G, et al. Knockdown of Bcl-2-associated athanogene-3 can enhance the efficacy of BGJ398 via suppressing migration and inducing apoptosis in gastric cancer[J]. Digestive Diseases and Sciences, 2021, 66(9): 3036-3044.
Protokoll (Protocol)
| Cell experiment [1]: | |
Cell lines | SKOV3ip1 cells |
Preparation Method | To measure cell viability of spheroid cultures, SKOV3ip1 cells (5 × 104) were seeded in ultra-low attachment 24-well plates and incubated overnight. BGJ398 were then added, and the cells were incubated for an additional 72 hours. Cells were harvested from each well and transferred to a regular 24-well plate for an additional 12 hours. Attached, live cells were stained with 0.2% crystal violet solution for 20 minutes with gentle agitation. The stained cells were washed with distilled water. For colorimetric analysis, the crystal violet dye was extracted with 1% SDS/PBS, and absorbance was measured at 570nm using an EMax PLUS microplate reader. |
Reaction Conditions | 0.3125-5µM; 72h |
Applications | The survival rate of SKOV3ip1 cells in spheroid culture was significantly reduced after BGJ398 treatment. |
| Animal experiment [2]: | |
Animal models | TMK-1 cells xenograft mice model |
Preparation Method | Cancer cells (1 × 106) were injected subcutaneously into the right flank of 6- to 8-week-old athymic nude mice. Mice were randomly assigned to either a control or treatment group. When tumors reached approximately 80mm3, BGJ398 (10mg/kg, administered by oral gavage) was initiated. Tumor diameters were measured, and volumes were calculated (width2 × length × 0.5). Tumors were excised, weighed, and processed for subsequent experiments. |
Dosage form | 10mg/kg; po; 20d |
Applications | Treatment with BGJ398 significantly inhibited tumor growth. |
References: | |
Produktdokumente (Product Documents)
Purity:>99.50%Appearance:A solid
Chemische Eigenschaften (Chemical Properties)
CAS-Nr.
872511-34-7
Synonyme
Infigratinib, NVP-BGJ398
Chemischer Name
3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-[6-[4-(4-ethylpiperazin-1-yl)anilino]pyrimidin-4-yl]-1-methylurea
SMILES
CCN1CCN(CC1)C2=CC=C(C=C2)NC3=CC(=NC=N3)N(C)C(=O)NC4=C(C(=CC(=C4Cl)OC)OC)Cl
Summenformel
C26H31Cl2N7O3
Molekulargewicht
560.48
Löslichkeit
≥ 7mg/mL in DMSO with gentle warming
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.
Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit
g/mol
Reviews
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