| S7818 |
Pexidartinib (PLX3397)
|
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.
|
-
Nat Commun, 2025, 16(1):6779
-
Nat Commun, 2025, 16(1):4590
-
Mol Ther, 2025, S1525-0016(25)00871-8
|
|
| S1010 |
BIBF 1120 (Nintedanib)
|
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.
|
-
Nat Commun, 2025, 16(1):471
-
Cell Death Dis, 2025, 16(1):196
-
Eur J Pharmacol, 2025, 1005:178058
|
|
| S7397 |
Sorafenib (BAY 43-9006)
|
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.
|
-
Mol Cancer, 2025, 24(1):34
-
Nat Commun, 2025, 16(1):509
-
Adv Sci (Weinh), 2025, 12(30):e04372
|
|
| S1119 |
Cabozantinib (XL184)
|
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.
|
-
Nat Commun, 2025, 16(1):509
-
Cell Death Differ, 2025, 10.1038/s41418-025-01510-x
-
Cell Death Dis, 2025, 16(1):76
|
|
| E7073 |
Rigosertib
|
Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle. Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM.
|
|
|
| S4487 |
Gilteritinib hemifumarate
|
Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
|
|
|
| S1040 |
Sorafenib Tosylate (BAY 43-9006)
|
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.
|
-
Int J Oncol, 2025, 67(3)72
-
Nature, 2024, 629(8013):927-936
-
Cell Mol Life Sci, 2024, 81(1):238
|
|
| S7781 |
Sunitinib (SU-11248)
|
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.
|
-
Cancer Cell, 2025, 43(4):776-796.e14
-
Mol Cancer, 2025, 24(1):179
-
J Exp Clin Cancer Res, 2025, 44(1):290
|
|
| S1042 |
Sunitinib (SU11248) Malate
|
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.
|
-
Nat Commun, 2025, 16(1):7853
-
CNS Neurosci Ther, 2025, 31(12):e70696
-
Sci Rep, 2025, 15(1):35889
|
|
| S1526 |
Quizartinib (AC220)
|
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.
|
-
Signal Transduct Target Ther, 2025, 10(1):222
-
Leukemia, 2025, 39(9):2152-2162
-
EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2
|
|