For research use only. Not for therapeutic Use.
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib also targets to CSF1R and c-KIT with IC50s of 8 nM and 14 nM, respectively. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension[1][2].
Seralutinib (GB002) (two-week treatment, delivered by inhalation) significantly reduces right ventricular systolic pressure and mean pulmonary artery pressure. Hemodynamic changes are accompanied by reduced pulmonary arteriole muscularization and restoration of BMPR2 protein expression in the lung lobes in Seralutinib (GB002)-treated animals. Seralutinib (GB002) is well tolerated[1].
Seralutinib-mediated inhibition of lung PDGFRα/β phosphorylation in healthy Sprague Dawley rats immediately post inhalation[2].
Seralutinib dose- and time-dependently induces lung BMPR2 protein expression[2].
| Catalog Number | I036228 |
| CAS Number | 1619931-27-9 |
| Synonyms | N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)pyrazin-2-yl]amino]ethyl]phenyl]-5-methylpyridine-3-carboxamide |
| Molecular Formula | C27H27N5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C27H27N5O3/c1-17-10-21(14-28-13-17)27(33)31-22-7-5-6-19(11-22)18(2)30-26-16-29-15-23(32-26)20-8-9-24(34-3)25(12-20)35-4/h5-16,18H,1-4H3,(H,30,32)(H,31,33)/t18-/m0/s1 |
| InChIKey | JHJNPOSPVGRIAN-SFHVURJKSA-N |
| SMILES | CC1=CC(=CN=C1)C(=O)NC2=CC=CC(=C2)C(C)NC3=NC(=CN=C3)C4=CC(=C(C=C4)OC)OC |
| Reference | [1]. Robert P. Frantz1, et.al. Phase 2 Clinical Study to Evaluate the Efficacy and Safety of Inhaled GB002 (Seralutinib) for the Treatment of World Health Organization Group 1 Pulmonary Arterial Hypertension [2]. Anna Galkin, et al. Abstract 11102: Gb002, A Novel Inhaled Pdgfr Kinase Inhibitor, Demonstrates Efficacy in the Su5416 Hypoxia Rat Model of Pulmonary Arterial Hypertension (pah). Circulation. 2019;140:A11102. [3]. Anna Galkin, et al. Pharmacologic Characterization of GB002, a Novel Inhaled PDGFR Kinase Inhibitor in Development for Pulmonary Arterial Hypertension (PAH). |
