PRN-1371
- Product Name
- PRN-1371
- CAS No.
- 1802929-43-6
- Chemical Name
- PRN-1371
- Synonyms
- PRN1371;PRN-1371;PRN1371 ，S8578;PRN1371, 10 mM in DMSO;8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one;8-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one(WX135248);Pyrido[2,3-d]pyrimidin-7(8H)-one, 6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)-8-[3-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]propyl]-;inhibit,CSF1R,PRN 1371,Inhibitor,colony stimulating factor 1 receptor,c-Fms,CSF-1R,FGFR,CSF-1 receptor,Fibroblast growth factor receptor,PRN1371,PRN-1371
- CBNumber
- CB63170401
- Molecular Formula
- C26H30Cl2N6O4
- Formula Weight
- 561.46
- MOL File
- 1802929-43-6.mol
PRN-1371 Property
- Boiling point:
- 771.7±70.0 °C(Predicted)
- Density
- 1.341±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:15.0(Max Conc. mg/mL);26.0(Max Conc. mM)
- form
- A solid
- pka
- 6.88±0.10(Predicted)
- color
- White to off-white
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-7485
- Product name
- PRN1371
- Purity
- 99.72%
- Packaging
- 1mg
- Price
- $90
- Updated
- 2021/12/16
- Product number
- CS-7485
- Product name
- PRN1371
- Purity
- 99.72%
- Packaging
- 5mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- CS-7485
- Product name
- PRN1371
- Purity
- 99.72%
- Packaging
- 10mg
- Price
- $500
- Updated
- 2021/12/16
- Product number
- CS-7485
- Product name
- PRN1371
- Purity
- 99.72%
- Packaging
- 50mg
- Price
- $1500
- Updated
- 2021/12/16
- Product number
- CS-7485
- Product name
- PRN1371
- Purity
- 99.72%
- Packaging
- 100mg
- Price
- $2100
- Updated
- 2021/12/16
PRN-1371 Chemical Properties,Usage,Production
Uses
PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively[1].
in vivo
PK studies of PRN1371 in rat, dog, and cynomolgus monkey show rapid iv clearance in all species. PRN1371 shows rapid clearance (Cl=160 mL per min per kg), yet dosing po (20 mg/kg) demonstrates high oral exposure (AUC=4348 h·ng/mL) and a reasonable half-life (t1/2=3.8 h). Low levels of pFGFR2 confirms the ability of PRN1371 to block FGFR2 activity in tumor tissue. PRN1371 induces a dose-dependent reduction in tumor volume and up to 68% tumor growth inhibition at the highest dose of 10 mg/kg b.i.d. following 27 days of treatment. All doses are well tolerated with no significant body weight loss. PRN1371 free base has been administered orally once daily as powder in a capsule on a 28-day continuous schedule. Human plasma concentrations for doses ranging from 15 to 35 mg confirm good oral exposure, rapid systemic clearance, no accumulation from day 1 to day 15, and a dose-dependent increase in AUC. Serum phosphate, a pharmacodynamic marker of FGFR inhibition, is increased for all doses studied and shows a dose-dependent increase between 20 and 35 mg, despite the administration of prophylactic phosphate binders[1].
IC 50
FGFR1: 0.6 nM (IC50); FGFR2: 1.3 nM (IC50); FGFR3: 4.1 nM (IC50); FGFR4: 19.3 nM (IC50); CSF1R: 8.1 nM (IC50)
References
[1] Brameld KA, et al. Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. J Med Chem. 2017 Aug 10;60(15):6516-6527. DOI:10.1021/acs.jmedchem.7b00360
PRN-1371 Preparation Products And Raw materials
Raw materials
Preparation Products
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