Pemigatinib
Binding Mode- Product Name
- Pemigatinib
- CAS No.
- 1513857-77-6
- Chemical Name
- Pemigatinib
- Synonyms
- IBI-375;INCB54828;INCB-54828;INCB 54828;INCB-054828;Pemigatinib;Pemigatinib, 10 mM in DMSO;Terbufos Impurity 14 (Ethion);3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholinomethyl)-3,4-dihydro-1H-pyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2(7H)-one;INCB 054828,Fibroblast growth factor receptor,INCB-054828,inhibit,cholangiocarcinoma,Orally,Pemigatinib,FGFR,Inhibitor,antineoplastic
- CBNumber
- CB54796678
- Molecular Formula
- C24H27F2N5O4
- Formula Weight
- 487.5
- MOL File
- 1513857-77-6.mol
Pemigatinib Property
- Boiling point:
- 697.6±55.0 °C(Predicted)
- Density
- 1.44±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:40.0(Max Conc. mg/mL);82.05(Max Conc. mM)
- form
- A crystalline solid
- pka
- 11.56±0.40(Predicted)
- color
- White to light yellow
- InChIKey
- HCDMJFOHIXMBOV-UHFFFAOYSA-N
- SMILES
- C1(=O)N(C2=C(F)C(OC)=CC(OC)=C2F)CC2=CN=C3NC(CN4CCOCC4)=CC3=C2N1CC
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0039499
- Product name
- Pemigatinib
- Purity
- 99.88%
- Packaging
- 5mg
- Price
- $120
- Updated
- 2021/12/16
- Product number
- CS-0039499
- Product name
- Pemigatinib
- Purity
- 99.88%
- Packaging
- 10mg
- Price
- $190
- Updated
- 2021/12/16
- Product number
- CS-0039499
- Product name
- Pemigatinib
- Purity
- 99.88%
- Packaging
- 25mg
- Price
- $350
- Updated
- 2021/12/16
- Product number
- CS-0039499
- Product name
- Pemigatinib
- Purity
- 99.88%
- Packaging
- 50mg
- Price
- $550
- Updated
- 2021/12/16
- Product number
- CS-0039499
- Product name
- Pemigatinib
- Purity
- 99.88%
- Packaging
- 100mg
- Price
- $950
- Updated
- 2021/12/16
Pemigatinib Chemical Properties,Usage,Production
Binding Mode
Pemigatinib binds to the inactive conformation
of FGFR1 with the activation loop adopting a DFG-in
conformation (type I1/2 inhibitor). The
pyrrolopyridine moiety forms two hydrogen bonds
with the NH and the carbonyl of Ala564 in the hinge
region (Figs. 3, 4). The difluoromethoxyphenyl ring,
which is perpendicular relative to the tricyclic ring, fits
the specificity pocket containing the gatekeeper
residue Val561. One of the methoxy oxygen atoms
hydrogen bonds to the backbone NH of Asp641. The
terminal morpholine extends towards the solventfront region, and makes only minor contacts with the
protein.
Uses
Pemigatinib is a potent inhibitor of FGFRs for the treatment of cholangiocarcinoma.
Indications
Pemigatinib is indicated for the treatment of previously treated adult patients with unresectable locally advanced or metastatic cholangiocarcinoma (CCA) who have been identified by an FDA-approved test for the presence of fibroblast growth factor receptor 2 (FGFR2) fusions or other rearrangements.
brand name
Pemazyre
General Description
Class: receptor tyrosine kinase; Treatment: metastatic cholangiocarcinoma; Other name: INCB054828; Elimination half-life = 15 h; Protein binding = 90.6%
Synthesis
Removal of the acetaldehyde protecting group in compound 284 under acidic conditions afforded aldehyde 285. Reductive amination of aldehyde 285 with aniline 286 gave benzylamine 287. Benzylamine 287 reacted with isocyanate 288 to form the desired urea 289. In the presence of a strong base, LHMDS (lithium dimethylsilane), compound 289 underwent intramolecular cyclization to displace the adjacent chlorine atom to yield azatricyclic compound 290. Conventional hydrolysis to remove the benzenesulfonyl group completed the construction of pemitinib, affording the final product in good yield.
target
Primary targets: Pan-FGFR
IC 50
FGFR1/2/3/4 IC 50 = 0.4, 0.5, 1, 30 nM
Pemigatinib Preparation Products And Raw materials
Raw materials
Preparation Products
Pemigatinib Suppliers
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View Lastest Price from Pemigatinib manufacturers
- Product
- Pemigatinib 1513857-77-6
- Price
- US $0.00/g
- Min. Order
- 1g
- Purity
- More Than 99%
- Supply Ability
- 100kg/Month
- Release date
- 2024-07-24
- Product
- Pemigatinib 1513857-77-6
- Price
- US $0.00-0.00/kg
- Min. Order
- 1kg
- Purity
- 99%, Single impurity＜0.1
- Supply Ability
- 1 ton
- Release date
- 2023-12-29
- Product
- Pemigatinib 1513857-77-6
- Price
- US $0.00-0.00/mg
- Min. Order
- 10mg
- Purity
- 98%
- Supply Ability
- 50kg
- Release date
- 2023-02-09