Catalog No.
Product Name
Application
Product Information
Citations
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IRAK4 inhibitor
PF-06650833 is an inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4). -
ITK inhibitor
PF 06465469 is a potent the nonreceptor tyrosine kinase Itk (IL-2 inducible T-cell kinase) inhibitor. It also inhibits BTK. -
Itk inhibitor
GSK-2250665A is a Itk inhibitor with pKi = 9.2, it Exhibits selectivity for Itk over Aurora B kinase and Btk (pIC50 values are 6.4 and 6.5, respectively) and a panel of other kinases. Inhibits IFNγ production in PBMCs. -
VEGFR-2 inhibitor
Apatinib mesylate(YN968D1 mesylate) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 with an IC50 of 1 nM.
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multi-targeted tyrosine kinase inhibitor
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities. -
multi-targeted receptor tyrosine kinase inhibitor
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Wei Kang Cheng, .et al. , Microvasc Res, 2022, Feb 11;142:104341 PMID: 35157839
- Sodium succinate dibasic is an inhibitor of multiple receptor tyrosine kinases. Sodium succinate dibasic is known to be a potent inhibitor of Met, Flt-1 (VEGFR1), Flk-1 (VEGFR2), Flt-3 (VEGFR3), Ron, and Tie-2. Sodium succinate dibasic has been observed to inhibit Met (c-Met)-driven tumor cell and non-c-Met driven tumor cell (HCT116 and MDA-MB-231) proliferation. This product has also been observed to effectively inhibit c-Met phosphorylation and its downstream signaling pathways in serum starved MKN45 cells, as well as inducing apoptosis in these cells.
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ALK inhibitor
Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively.- Sang-Yun Lee, .et al. , J Exp Clin Cancer Res, 2023, Nov 22;42(1):309 PMID: 37993887
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EGFR inhibitor
Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.- Hui-Ju Huang, .et al. , Exp Biol Med (Maywood), 2025, May 15;250:10554 PMID: 40444141
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FLT3/AXL inhibitor
Gilteritinib hemifumarate is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively. -
EGFR inhibitor
Osimertinib dimesylate (AZD-9291 dimesylate) is an irreversible and mutant selective EGFR inhibitor with IC50s of 12 and 1 nM against EGFRL858R and EGFRL858R/T790M, respectively. -
c-Met inhibitor
JNJ-38877618 is a novel potent, highly selective, orally bioavailable c-Met tyrosine kinase inhibitor with Kd of 1.2, 2.1 and 21 nM for WT, M1250T and Y1235D mutants MET, respectively. -
c-Met inhibitor
Glumetinib (SCC244) is a potent and highly selective c-Met kinase inhibitor with an IC50 of 0.42 nM. Glumetinib shows antitumor activity and a superior safety margin. -
CSF-1R inhibitor
TE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis. -
c-FMS inhibitor
c-Fms-IN-9 is a c-FMS inhibitor extracted from patent WO2014145023A1, Compound Example 7. c-Fms-IN-9 inhibits unphosphorylated c-FMS kinase (uFMS) and uKIT with IC50s of <0.01 μM and 0.1-1 μM, respectively. -
c-KIT inhibitor
c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively. -
c-KIT T670I mutant inhibitor
CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM. -
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. -
FLT-3 ITD degrader
PROTAC FLT-3 degrader 1 is an FLT-3 internal tandem duplication (ITD) degrader with an IC50 0.6 nM. Anti-proliferative activity; apoptosis induction. -
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.
