A PDGFR, c-Kit, and CSF1R inhibitor
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Seralutinib

Item No. 37754

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-[(1S)-1-[[6-(3,4-dimethoxyphenyl)-2-pyrazinyl]amino]ethyl]phenyl]-5-methyl-3-pyridinecarboxamide
CAS Number
1619931-27-9
Synonyms
  • GB002
  • PK 10571
Molecular Formula
C27H27N5O3
Formula Weight
469.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 25 mg/mlEthanol: 10 mg/ml
λmax
273 nm
SMILES
COC1=C(OC)C=CC(C2=NC(N[C@H](C3=CC(NC(C4=CN=CC(C)=C4)=O)=CC=C3)C)=CN=C2)=C1
InChi Code
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
InChi Key
JHJNPOSPVGRIAN-SFHVURJKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $107

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    10 mg

    $204

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    25 mg

    $481

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    50 mg

    $801

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    Product Description

    Seralutinib is an inhibitor of PDGFR, c-Kit, and colony stimulating factor 1 receptor (CSF1R).1 It inhibits PDGF-BB-induced phosphorylation of ERK in PDGFRα-dependent H1703 human lung epithelial cells, human pulmonary arterial smooth muscle cells (HPASMCs), which express PDGFRα and PDGFRβ, and human lung fibroblasts (HLFs), which express higher levels of PDGFRβ than PDGFRα (IC50s = 74, 49, and 62 nM, respectively). Seralutinib also inhibits stem cell factor-induced c-Kit autophosphorylation in human pulmonary endothelial cells (HPAECs) and M-CSF-induced CSF1R phosphorylation in human primary differentiated macrophages (IC50s = 7.8 and 14.4 nM, respectively). It inhibits the proliferation of H1703 cells and PDGF-BB-induced HPASMCs and HLFs (IC50s = 32, 33, and 29 nM, respectively). Seralutinib (2.5 mg/kg) prevents increases in pulmonary artery systolic pressure in a rat model of pulmonary arterial hypertension induced by monocrotaline (Item No. 16666) pneumonectomy when administered via passive inhalation.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Galkin, A., Sitapara, R., Clemons, B., et al. Inhaled seralutinib exhibits potent efficacy in models of pulmonary arterial hypertension. Eur. Respir. J. 60(6), 2102356 (2022).