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).
Products are for research use only. Not for human use. We do not sell to patients.
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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Citations
1 publicationsPublications from researchers using this productDescription
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.
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: | |
Product Documents
Purity:>99.50%Appearance:A solid
Chemical Properties
CAS No.
872511-34-7
Synonyms
Infigratinib, NVP-BGJ398
Chemical 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
Molecular Formula
C26H31Cl2N7O3
Molecular Weight
560.48
Solubility
≥ 7mg/mL in DMSO with gentle warming
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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