Infigratinib
Uses- Product Name
- Infigratinib
- CAS No.
- 872511-34-7
- Chemical Name
- Infigratinib
- Synonyms
- BGJ-398;Infligratinib;BGJ;CS-218;BGJ 398;NVP-BGJ398;Infigratinib;Transcrocetinate;NVP-BGJ398, >=98%;BGJ398 (NVP-BGJ398)
- CBNumber
- CB52589643
- Molecular Formula
- C26H31Cl2N7O3
- Formula Weight
- 560.48
- MOL File
- 872511-34-7.mol
Infigratinib Property
- Melting point:
- >211°C (dec.)
- Boiling point:
- 747.9±60.0 °C(Predicted)
- Density
- 1.354
- storage temp.
- -20°C
- solubility
- Soluble in DMSO (up to 5 mg/ml)
- form
- White solid.
- pka
- 11.02±0.70(Predicted)
- color
- White
- Stability:
- Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
- InChIKey
- QADPYRIHXKWUSV-UHFFFAOYSA-N
- SMILES
- N(C1C=C(NC2=CC=C(N3CCN(CC)CC3)C=C2)N=CN=1)(C)C(NC1=C(Cl)C(OC)=CC(OC)=C1Cl)=O
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P271Use only outdoors or in a well-ventilated area.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P312Call a POISON CENTER or doctor/physician if you feel unwell.
P321Specific treatment (see … on this label).
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
P403+P233Store in a well-ventilated place. Keep container tightly closed.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 19157
- Product name
- BGJ398
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 19157
- Product name
- BGJ398
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $120
- Updated
- 2024/03/01
- Product number
- 19157
- Product name
- BGJ398
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $191
- Updated
- 2024/03/01
- Product number
- 19157
- Product name
- BGJ398
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $313
- Updated
- 2024/03/01
- Product number
- B367000
- Product name
- BGJ398
- Packaging
- 200mg
- Price
- $425
- Updated
- 2021/12/16
Infigratinib Chemical Properties,Usage,Production
Uses
BGJ 398 is a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Description
NVP-BGJ398 (872511-34-7) is a potent and selective pan-FGFR inhibitor (IC50?= 0.9nM, 1.4 nM, 1.0 nM, and 60 nM for FGFR1,2,3,4 respectively).1? It has also been used in a mouse model of Achondroplasia (most common form of dwarfism) to correct pathological hallmarks of this condition.
Uses
BGJ 398 is a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Definition
ChEBI: BGJ-398 is a member of the class of phenylureas that is urea in which a hydrogen attached to one of the nitrogens is replaced by a 2,6-dichloro-3,5-dimethoxyphenyl group, while the hydrogens attached to the other nitrogen are replaced by a methyl group and a 6-{[4-(4-ethylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl group. It is a potent and selective fibroblast growth factor receptor inhibitor. It has a role as a fibroblast growth factor receptor antagonist and an antineoplastic agent. It is an aminopyrimidine, a N-arylpiperazine, a N-alkylpiperazine, a dichlorobenzene and a member of phenylureas.
Indications
Infigratinib is approved by the USFDA for the treatment of previously treated patients with advanced or metastatic cholangiocarcinoma carrying FGFR2 fusion or rearrangement. Its inhibitory effect on FGFR helps reduce the proliferation of tumor cells, especially for cholangiocarcinoma patients with abnormal activation of the FGFR pathway. It is used as an oral drug, which provides convenience for patients.
brand name
Truseltiq
General Description
Class: receptor tyrosine kinase; Treatment: cholangiocarcinoma; Other name: NVP-BGJ398; Elimination half-life = 34 h; Protein binding = 96.8%
Mechanism of action
Infigratinib works at the biochemical and cellular levels by highly selectively inhibiting the activity of FGFR1, FGFR2, FGFR3, and FGFR4. Activation of the FGFR pathway is associated with the proliferation of malignant cancer cells, therefore, inhibition of FGFR-specific kinases can effectively reduce tumor cell proliferation.
Side effects
Side effects of infigratinib may include stomatitis, fatigue, decreased appetite, high blood pressure, and elevated liver enzyme levels.
Synthesis
Infigratinib was synthesized in a modular and polymeric manner by combining three building blocks. Piperidine-substituted aniline 32.4 was prepared by SNAr reaction of piperidine 32.1 and bromonitrobenzene 32.2 at 80°C followed by nitro reduction (Figure 1a). 2,6-Dichloro-3,5-dimethoxyaniline (32.6) was obtained from commercially available 3,5-dimethoxyaniline (32.5) in three steps (acylation, chlorination, and hydrolysis) (Figure 1b), and 6-chloro-N-methylpyrimidin-4-amine (32.8) was prepared by SNAr reaction of dichloropyrimidine 32.7 with methylamine (Figure 1c).
Aniline 32.4 and chloropyrimidine 32.8 were SNAr reacted to generate arylmethylamine 32.9, thereby assembling Infigratinib (Figure 2). The aniline derivative 32.6 was converted in situ to the corresponding isocyanate and combined with 32.9 to form a urea bond, completing the synthesis of Infigratinib.
target
FGFR1
IC 50
FGFR1~4 IC50 = 0.9, 1.4, 1.0, and 60 nM; VEGFR2 IC50 = 180 nM
References
[1] Discovery of 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-(6-{[4-(4-ethyl-1-piperazinyl)phenyl]amino}-4-pyrimidinyl)-1-methylurea (NVP-BGJ398), a Potent and Selective Inhibitor of the Fibroblast Growth Factor Receptor Family of Receptor Tyrosine Kinase
[2] DAVIDE KOMLA-EBRI. Tyrosine kinase inhibitor NVP-BGJ398 functionally improves FGFR3-related dwarfism in mouse model.[J]. The Journal of clinical investigation, 2016: 1871-1884. DOI:10.1172/jci83926
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View Lastest Price from Infigratinib manufacturers
- Product
- Infigratinib 872511-34-7
- Price
- US $0.00/Bag
- Min. Order
- 1Bag
- Purity
- ＞99%
- Supply Ability
- 1kg
- Release date
- 2025-06-29
- Product
- Infigratinib (BGJ398) 872511-34-7
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- 98% HPLC
- Supply Ability
- 1kg
- Release date
- 2023-08-02
- Product
- 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-[6-[[4-(4-ethylpiperazin-1-yl)phenyl]amino]pyrimidin-4-yl]-1-methylurea 872511-34-7
- Price
- US $2.00/KG
- Min. Order
- 1g
- Purity
- 98%min
- Supply Ability
- ask
- Release date
- 2020-01-08