| S7818 |
Pexidartinib (PLX3397)
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Pexidartinib (PLX3397) is an oral, potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, Kit (c-Kit), and FLT3 with IC50 of 20 nM, 10 nM and 160 nM, respectively. This compound induces apoptosis and necrosis with antitumor activity. Phase 3.
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Glia, 2026, 74(3):e70120
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Nat Commun, 2025, 16(1):6779
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Nat Commun, 2025, 16(1):4590
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| S1010 |
BIBF 1120 (Nintedanib)
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Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.
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Cancer Biology & Medicine, November 19, 2025, 20250275
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Thorax, February 18, 2026, thorax-2025-223325
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Drug Design, Development and Therapy, February 18, 2022, 397-411
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| S7397 |
Sorafenib (BAY 43-9006)
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Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
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J Hepatocell Carcinoma, 2026, 13:572919
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Mol Cancer, 2025, 24(1):34
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Nat Commun, 2025, 16(1):509
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| S1119 |
Cabozantinib (XL184)
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A potent VEGFR2 inhibitor with IC50 of 0.035 nM, Cabozantinib (XL184) also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. It induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.
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Cell Reports Medicine, September 20, 2022, 100659
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Redox Biology, October 21, 2023, 102945
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Hepatology Communications, November 8, 2023, e0313
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| S4487 |
Gilteritinib hemifumarate
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Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
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| S1040 |
Sorafenib Tosylate (BAY 43-9006)
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Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
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Int J Oncol, 2025, 67(3)72
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Nature, 2024, 629(8013):927-936
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Cell Mol Life Sci, 2024, 81(1):238
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| S7781 |
Sunitinib (SU-11248)
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Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.
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Cancer Cell, 2025, 43(4):776-796.e14
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Mol Cancer, 2025, 24(1):179
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J Exp Clin Cancer Res, 2025, 44(1):290
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| S1042 |
Sunitinib (SU11248) Malate
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Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.
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Nat Commun, 2025, 16(1):7853
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CNS Neurosci Ther, 2025, 31(12):e70696
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Sci Rep, 2025, 15(1):35889
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| S1526 |
Quizartinib (AC220)
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Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Quizartinib (AC220) induces apoptosis of tumor cells. Phase 3.
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Signal Transduct Target Ther, 2025, 10(1):222
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Leukemia, 2025, 39(9):2152-2162
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EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2
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| S2194 |
R406
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R406(R406 besylate) is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 induces apoptosis. Phase 1.
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Aging (Albany NY), May 7, 2020, 8221-8240
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eLife, April 30, 2020, e56656
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Cancer Research, April 15, 2017, 1818-1830
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