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Catalog No.
Product Name
Application
Product Information
Citations
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EGFR inhibitor
EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity. -
EGFR inhibitor
Mutated EGFR-IN-2 (compound 91) is a mutant-selective EGFR inhibitor extracted from patent WO2017036263A1, which potently inhibits single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M (IC50=??1nM) and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. Mutated EGFR-IN-2 shows anti-tumor antivity. -
FGFR1/DDR2 inhibitor
FGFR1/DDR2 inhibitor 1 is an inhibitor of fibroblast growth factor receptor 1 (FGFR1) and discoindin domain receptor 2 (DDR2), with IC50 values of 31.1 nM, 108.4 nM and 3.2 nM for FGFR1, KG-1, and DDR2, respectively. -
CSF-1R, c-FMS Type II inhibitor
c-Fms-IN-8 (compound 4a) is a colony stimulating factor-1 receptor (CSF-1R, c-FMS) Type II inhibitor, with an IC50 of 9.1 nM. -
CSF1R inhibitor
PLX5622 is a highly selective brain penetrant and oral active CSF1R inhibitor with an Ki of 5.9 nM, for extended and specific microglial elimination, preceding and during pathology development.- Sang Hwan Lee, .et al. , Brain, 2024, Aug 28:awae221 PMID: 39194073
- Ilija Brizic, .et al. , Research Square, 2024, October 3rd
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VEGFA inhibitor
PTC299 is a potent, orally bioavailable VEGFA inhibitor, targets dihydroorotate dehydrogenase (DHODH), resulting in cell growth inhibition and differentiation in leukemias, including acute myeloid leukemia, linking DHODH regulation and stress-induced VEGFA and angiogenesis. -
FMS inhibitor
c-Fms-IN-10 is the derivative of thieno [3,2-d] pyrimidine, an kinase inhibitor of FMS (Colony stimulating factor-1 receptor, CSF-1R) with IC50 of 2 nM. c-Fms-IN-10 has anti-tumor activity. -
ITK inhibitor
ITK inhibitor 2 is a interleukin-2-inducible T-cell kinase (ITK) inhibitor extracted from patent WO2011065402A1, compound 4, with an IC50 of 2 nM. -
TKI inhibitor
Selitrectinib (LOXO-195) is a next-generation TRK kinase inhibitor (TKI), with IC50s of 0.6 nM, <2.5 nM for TRKA and TRKC respectively. -
c-Met inhibitor
c-Met-IN-2 is a potent, selective and orally available c-Met inhibitor, with an IC50 of 0.6 nM, with antitumor activity. -
cFMS inhibitor
c-Fms-IN-7 is a cFMS inhibitor extracted from patent WO2011079076A1, example159, has an IC50 of 18.5 nM. -
c-FMS inhibitor
c-Fms-IN-6 is a potent inhibitor of c-FMS, with an IC50 of ??10 nM for unphosphorylated c-FMS, also weakly inhibits unphosphorylated c-KIT and PDGFR (IC50, > 1 μM). Used in the research of autoimmune diseases. -
FGFR4 inhibitor
Roblitinib (FGF-401; Compound Example 83) is a highly selective and potent FGFR4 inhibitor with an IC50 of 1.9 nM. Roblitinib has antitumor activity. -
KIT and PDGFRA inhibitor
Avapritinib (BLU-285) is a highly potent, selective, and orally bioavailable KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. -
KIT and PDGFRA switch-control inhibitor
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. -
EGFR inhibitor
TAS6417 is an EGFR inhibitor and an efficacious drug candidate for patients with NSCLC, with IC50 values ranging from 1.1-8.0 nM. -
IRAK4 inhibitor
IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor with an IC50 of 7 nM. -
type II PDGFRα kinase inhibitor
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively. -
ALK/MET inhibitor
Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. -
ROS1/TRK inhibitor
Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor. -
SRC inhibitor
CSF1R-IN-2 (compound 5) is an oral-active inhibitor of SRC, MET and c-FMS, with IC50 values of 0.12 nM, 0.14 nM and 0.76 nM for SRC, MET and c-FMS respectively.
