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VEGFR/FGFR/EGFR inhibitor?€?
SU-5402 is a potent and selective vascular endothelial growth factor receptor (VEGFR) and fibroblast growth factor receptor (FGFR) inhibitor (IC50 values are 0.02, 0.03, 0.51 and > 100 μM at VEGFR2, FGFR1, PDGFRβ and EGFR respectively). -
HER2/ErbB2 inhibitor
CP-724714 is an orally available, small molecule, potent HER-2 tyrosine kinase inhibitor that inhibits HER2 kinase (IC50 3.8 ng/ml) .- Yu Muta, .et al. , Nat Commun, 2018, 9: 2174 PMID: 29872037
- Gina M. Sizemore, .et al. , Nat Commun, 2018, 9: 2783 PMID: 30018330
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ALK Inhibitor
TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant).- Yue Guo, .et al. , Cell Biosci, 2022, Dec 30;12(1):210 PMID: 36585695
- Li Li, .et al. , Leukemia Res, 2019, 78:12-20 PMID: 30660961
- Li T, .et al. , Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
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EGFR inhibitor
Dacomitinib (PF299804, PF299) is a potent, orally available, irreversible inhibitor of tyrosine kinase human epidermal growth factor receptors (HER) 1 (EGFR), HER2, and HER4.
- Yuji Uehara, .et al. , Lung Cancer, 2025, Apr:202:108479 PMID: 40088581
- Aya Hasan Alshammari, .et al. , Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
- Hamzehlou S, .et al. , Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Momeny M, .et al. , Cell Oncol (Dordr), 2019, Apr 25 PMID: 31025257
- Majid Momeny, .et al. , Sci Rep, 2017, 7: 4204 PMID: 28646172
- Fujita KI, .et al. , J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
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EGFR inhibitor
Poziotinib is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity.- Yuji Uehara, .et al. , Lung Cancer, 2025, Apr:202:108479 PMID: 40088581
- Ikei S Kobayashi, .et al. , Cells, 2021, 10(12): 3561 PMID: 34944068
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TGF-β/ALK5 inhibitor
A83-01 is a selective inhibitor of the transforming growth factor-beta type I receptor ALK5, the Nodal receptor ALK4, and the nodal receptor ALK7- Yuko Nagashima, .et al. , Sci Rep, 2026, Feb 25;16(1):7582 PMID: 41741551
- T Usui, .et al. , ResearchSquare, 2026, Feb 22
- Jin-Young Lee, .et al. , Mater Today Bio, 2026, Mar 19;38:103026 PMID: 41953717
- Yuko Nagashima, .et al. , Research Square, 2025, Sep 26
- Yuta Shinohara, .et al. , J Vet Med Sci, 2025, Feb 15;87(2):232-240 PMID: 39756955
- Yuko Nagashima, .et al. , Sci Rep, 2025, Feb 19;15(1):6108 PMID: 39972078
- Masayuki Fukumoto, .et al. , PLoS One, 2024, Dec 5;19(12):e0313312 PMID: 39636897
- Raghda Shahin, .et al. , Drug Metabolism and Pharmacokinetics, 2024, 4 December PMID: 40373539
- Kyunghyun Park, .et al. , Advanced Therapeutics, 2024, 7(6)
- Yuko Nagashima, .et al. , Research Square, 2024, June 4th
- Shota Mizuno, .et al. , Biol Pharm Bull, 2024, 47(1):120-129 PMID: 38171772
- Andreea Manole, .et al. , Cell Rep, 2023, Dec 26;42(12):113466 PMID: 38039131
- Claudia Z Han, .et al. , Immunity, 2023, Sep 12;56(9):2152-2171 PMID: 37582369
- Yomogi Shiota Sato, .et al. , Biomed Pharmacother, 2023, Sep;165:115079 PMID: 37413906
- Yomogi Sato, .et al. , Biomed Pharmacother, 2023, Jun;162:114651 PMID: 37030135
- Dan Zhao, .et al. , Poult Sci, 2022, Mar; 101(3): 101642 PMID: 35016046
- Anna Nakanishi, .et al. , Regen Ther, 2022, Sep 9;21:351-361 PMID: 36161099
- Amira Abugomaa, .et al. , Biomed Pharmacother, 2022, Oct;154:113597 PMID: 36030590
- Isamu Ogawa, .et al. , Biomaterials, 2022, Sep;288:121696 PMID: 36038421
- Mohamed Elbadawy, .et al. , Cancer Biol Ther, 2021, Jun 3;22(5-6):357-371 PMID: 34034619
- Mohamed Elbadawy, .et al. , Authorea, 2020, October 20
- Daichi Onozato, .et al. , Biol Pharm Bull, 2020, 43(7), 1088-1095 PMID: 32612071
- Amira Abugomaa, .et al. , Sci Rep, 2020, Jun 10;10(1):9393 PMID: 32523078
- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
- Kondo S, .et al. , Biol Open, 2020, Jan 9;9(1) PMID: 31919043
- Onozato D, .et al. , Drug Metab Dispos, 2018, Nov;46(11):1572-1580 PMID: 29615438
- Usui T, .et al. , Curr Protoc Toxicol, 2018, Feb 21;75:22.6.1-22.6.7 PMID: 29512123
- Kondo S, .et al. , Inflamm Res, 2018, Dec;67(11-12):975-984 PMID: 30317465
- Onozato D, .et al. , Stem Cells Dev, 2018, Aug 1;27(15):1033-1045 PMID: 29742964
- Tatsuya Usui, .et al. , Int J Mol Sci, 2018, Apr; 19(4): 1098 PMID: 29642386
- Tatsuya Usui, .et al. , Cancer Sci, 2017, Dec; 108(12): 2383-2392 PMID: 29024204
- Tatsuya Usui, .et al. , Physiol Rep, 2017, Jun; 5(12): e13318 PMID: 28642339
- Tatsuya Usui, .et al. , Stem Cells Int, 2016, 2016: 7053872 PMID: 28119740
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RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively.- Yunping Hu, .et al. , Cancer Lett, 2022, Oct 28;547:215867 PMID: 35985510
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Bcr-Abl inhibitor
Bafetinib ((INNO-406) is a dual Bcr-Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia.- Yusuke Kimata, .et al. , Life Sci Alliance, 2023, Feb 27;6(5):e202201657 PMID: 36849250
- Li T, .et al. , Oncogene, 2018, Nov;37(47):6180-6194 PMID: 30013190
- S. Dallari, .et al. , Nat Commun, 2017, 8: 14830 PMID: 28368000
- Andrea Haerzschel, .et al. , Ann Hematol, 2016, 95(12): 1979-1988 PMID: 27542958
- Magdalena Winiarska, .et al. , MAbs., 2014, 6(5): 1300-1313 PMID: 25517315
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EGFR inhibitor
Erlotinib hydrochloride is a reversible tyrosine kinase inhibitor, which acts on the epidermal growth factor receptor (EGFR).- Yuta Yamamoto, .et al. , J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Aikawa S, .et al. , Biochem Biophys Res Commun, 2017, Feb 26;484(1):202-208 PMID: 28073697
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EGFR Inhibitor
OSI-420 (Desmethyl Erlotinib,CP-473420) is an orally active EGFR tyrosin kinase inhibitor, which inhibits receptor tyrosine kinases (TKs) by inhibition of the intercellular domain .- Yuta Yamamoto, .et al. , J Pharm Anal, 2018, Apr; 8(2): 119-123 PMID: 29736298
- Janet L. Martin, .et al. , Breast Cancer Res, 2017, 19: 90 PMID: 28778177
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Vascular Disrupting Agent (VDA)
DMXAA (ASA404) is a tumor-vascular disrupting agent (tumor-VDA) that attacks the blood supply of a cancerous tumor to cause tumor regression.- Zhang X, .et al. , ACS Infect Dis, 2019, May 14 PMID: 31060350
- Bowei Liu, .et al. , Antiviral Res, 2017, Nov; 147: 37-46 PMID: 28982551
- Fang Guo, .et al. , Antimicrob Agents Chemother, 2017, Oct; 61(10): e00771-17 PMID: 28717041
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Apoptotic, antiproliferative and antiangiogenic agent
2-Methoxyestradiol is an apoptotic, antiproliferative and antiangiogenic agent. Induces p53-induced apoptosis via two pathways: activation of p38 and NF-κB; and activation of JNK and AP-1 leading to Bcl-2 phosphorylation. -
HER2 inhibitor
Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA. -
EGFR inhibitor
AST-6 is a novel irreversible inhibitor of the epidermal growth factor receptor 1 and 2, inhibits tumor growth both in vitro and in vivo -
c-Met inhibitor
BMS-794833 is a potent ATP competitive inhibitor to Met and VEGFR-2 with IC50 of 1.7 and 15 nmol. -
VEGFR inhibitor
Brivanib alaninate (BMS-582664) is a dual tyrosine kinase inhibitor of VEGFR and FGFR signaling. -
RTK inhibitor
Dovitinib is a small-molecule multitargeted receptor tyrosine kinase inhibitor, which inhibits Ba/F3 cells transformed to IL3 independence by ZNF198-FGFR1 or BCR-FGFR1 with IC50 values of 150 nM and 90 nM, respectively. -
EGFR inhibitor
Chrysophanic acid (Chrysophanol) blocks proliferation of colon cancer cells by inhibiting EGFR/mTOR pathway. -
EGFR, PKA,PKC inhibitor
Daphnetin is a coumarin analog that acts as an inhibitor of several protein kinases. It inhibits EGFR kinase (IC50 = 7.67 μM), PKA (IC50 = 9.33 μM), and PKC (IC50 = 25 μM), in vitro. The inhibition of EGFR kinase by daphnetin was competitive to ATP and non-competitive to the peptide substrate. Also acts as a potent antioxidant and anti-malarial agent. -
HER2 inhibitor
Lapatinib is a dual tyrosine kinase inhibitor which interrupts the HER2 growth receptor pathway. -
c-Met inhibitor
MGCD265 is a multitargeted tyrosine kinase inhibitor that binds to and inhibits the phosphorylation of several RTKs, including the c-Met receptor (HGFR); the Tek/Tie-2 receptor; VEGFR types 1, 2, and 3; and MST1R. -
VEGFR inhibitor
Motesanib, also known as AMG-706, is an orally administered multikinase inhibitor that selectively targets VEGF receptors, platelet-derived growth factor receptors, and Kit receptors. -
HER2/ErbB2 inhibitor
Mubritinib (TAK 165) is a potent EGFR and p34cdc2 inhibitor with IC50 of 6 nM and 0.2 μM, respectively. Mubritinib(TAK 165) also inhibits p33cdk2 and p33cdk5. -
Microtubule Inhibitor
NPI-2358 is a synthetic analog of NPI-2350, a natural product isolated from Aspergillus sp., which depolymerizes microtubules in A549 human lung carcinoma cells. -
EGFR inhibitor
PD153035 is an extremely potent and specific inhibitor of the tyrosine kinase activity of EGFR. -
Syk Inhibitor
R406 is an orally available spleen tyrosine kinase inhibitor with an IC50 of 41 nM. -
Syk Inhibitor
R935788 (Fostamatinib disodium) is a potent orally available inhibitor of Syk that inhibits tumor growth in the Eμ- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. -
RAF/VEGFR Inhibitor
RAF265 (CHIR-265) is an oral, highly selective RAF and VEGFR kinase inhibitor, which is to control or normalize VEGFR-2 along with the inhibition of B-raf and c-Raf mutation to prevent cancers. -
RAF/VEGFR Inhibitor
Raf265 derivative is a derivative of Raf265 that is an oral, highly selective RAF and VEGFR kinase inhibitor with IC50 of of 5 to 10 μM. -
FLT3 Inhibitor
Tandutinib (MLN518) inhibits the autophosphorylation of FLT3, c-KIT and PDGF receptor tyrosine kinases, thereby inhibiting cellular proliferation and inducing apoptosis. -
VEGFR-2 inhibitor
Telatinib (BAY 57-9352) is an orally available, small-molecule inhibitor of vascular endothelial growth factor receptors 2 and 3 (VEGFR-2/-3) and platelet-derived growth factor receptor β tyrosine kinases. -
HER2 Inhibitor
ARRY-380 is an ErbB-2 inhibitor that selectively binds to and inhibits the phosphorylation of ErbB-2, resulting in growth inhibition and death of ErbB-2-expressing tumor cells. -
EGFR, HER2 and VEGFR inhibitor
XL647 is an orally bioavailable small-molecule RTK inhibitor that binds to and inhibits several tyrosine receptor kinases that play major roles in tumor cell proliferation and tumor vascularization, including EGFR, HER2, ERBB2, VEGFR and EphB4. -
JAK2/FLT3 inhibitor
TG-101348 is an orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 with potential antineoplastic activity. -
VEGFR/c-Met/HGFR inhibitor
TAS-115 is a potent VEGFR and hepatocyte growth factor receptor (c-Met/HGFR)-targeted kinase inhibitor with IC50s of 30 and 32 nM for rVEGFR2 and rMET, respectively. -
multi-targeted kinase inhibitor
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. -
EGFR/T790M inhibitor
HS-10296 hydrochloride is an orally available and third-Generation inhibitor of epidermal growth factor receptor (EGFR)-activating mutations and T790M-resistant mutation with limited activity against wild-type EGFR.

