RK-20448 is an ATP-competitive inhibitor of Lck, Src, KDR/VEGF2R and Tie-2 with IC50 values of 0.24, 1.19, 10.74 and 5.85 µM, respectively. RK-20448 also inhibits BLK, Csk, Fyn and Lyn with IC50 values of 0.37, 4.27, 2.03 and 0.43 µM, respectively. RK-20448 is the cis isomer of A-419259 derivative with neuroprotective and PP2A activating activities. FTY720-Mitoxy has the property of targeting mitochondria. In addition, FTY720-Mitoxy protects neurons by reducing inflammatory responses and is used in the study of neurodegenerative diseases such as Parkinson's disease.

K882 (Compound 4e) is a Src inhibitor, with KD of 0.315 μM. K882 induces Apoptosis. K882 inhibits XIAP and Survivin. K882 inhibits the activation of PI3K/Akt/mTOR, Jak1/Stat3, Ras/MAPK signaling pathways. K882 shows anti-tumor activity against non-small cell lung cancer.

CGP062464 is an inhibitor of the tyrosine kinase c-Src (IC50: < 50 nM). CGP062464 can be used for research of osteoporosis and tumor-induced hypercalcemia.

Xanthinol is a potent modulator of tumor hemodynamics.

RPR-101511 is a 3-substituted quinoline derivative. RPR-101511 is a PDGF receptor tyrosine kinase inhibitor (IC50: 0.001-0.02 μM).

2-Methyl-3-phenylquinoxaline (compound 38) is a potent platelet-derived growth factor receptor tyrosine kinase (PDGF-RTK) inhibitor with modest inhibitory activity against PDGFR kinase in intact cells (IC50 greater than 100 μM).

DDN is a selective insulin receptor (Insulin Receptor) activator, an insulin sensitizer, and a glucose-lowering insulin mimetic with oral bioavailability. DDN can directly bind to the receptor kinase domain and induce Akt and ERK phosphorylation, and it can also enhance insulin's effect on glucose uptake. DDN significantly reduces blood glucose levels in wild-type and diabetic ob/ob and db/db mice.

Lomonitinib is a highly potent and selective pan-FLT3/IRAK4 inhibitor with antitumor activity. Lomonitinib is promising for research of myeloid leukemia.

HSN748 is a Ponatinib, and exhibits inhibitory activity against heparanase. Pixatimod free acid binds to the S1 receptor binding domain (RBD) of the SARS-CoV-2 virus, that inhibits SARS-CoV-2 isolate strains with EC50 of 2.4-13.8 µg/mL. Pixatimod free acid is an agonist for TLR9 signaling pathway, enhances the activity of dendritic cells (DCs), activates natural killer cells, and exhibits immunomodulatory and anti-tumor activities.

FW-1 is a type I inhibitor for FLT3 with IC50 of ca. 1 μM. FW-1 exhibits cytotoxicity in FLT3 mutated AML cell. FW-1 arrests the cell cycle at G0/G1 phase, and induces apoptosis in cell MV4-11 and MOLM-13.

Clifutinib (Compound 9e) is an orally active and selective internal tandem duplication mutation of FMS-like tyrosine kinase 3 (FLT3-ITD) inhibitor with an IC50 value of 15.1 nM. Clifutinib inhibits the activity of FLT3-ITD kinase and blocks the downstream RAS/MAPK, PI3K/AKT, and JAK/STAT5 signaling pathways of FLT3. Clifutinib induces apoptosis of acute myeloid leukemia (AML) cells with FLT3-ITD mutations. Clifutinib is promising for research of relapsed/refractory FLT3-ITD-positive acute myeloid leukemia.

CHEMBL4444839 is an inhibitor of FLT3 and can be used in the research of acute myeloid leukemia (AML).

CG-3-246 is a dual inhibitor of FLT3/BCL-2, with the Kds of 63 and 4.25 nM, respectibely. CG-3-246 plays an important role in acute myeloid leukemias research.

Siphonaxanthin is a keto-carotenoid with anti-angiogenic and anti-inflammatory activity, which is found in green algae. Siphonaxanthin upregulates the expression of death receptor 5 (DR5), induces cancer cell apoptosis, decreases the expression of Bcl-2, and activates caspase-3. Siphonaxanthin is also an inhibitor of FGFR-1. Siphonaxanthin inhibits the proliferation, migration, and tube formation of human umbilical vein endothelial cells (HUVECs), as well as the outgrowth of microvessels in the rat aortic ring. Siphonaxanthin is promising for research of diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.

PNU-145156E (FCE26644) is an angiogenesis inhibitor with anti-tumor activity. PNU-145156E inhibits the binding of bFGF to its receptor and inhibits bFGF-induced endothelial cell proliferation and motility.

BW710 is an orally active fibroblast growth factor receptor 2 (FGFR2) inhibitor. BW710 inhibits the proliferation of BaF3-FGFR2 cells with an IC50 of 2.8 nM. BW710 abolishes FGFR2 enzymatic activity and is selective against other 75 tyrosine kinases including FGFR1, FGFR3, and FGFR4 at 1 μM. BW710 suppresses the FGFR2 signaling and selectively inhibits FGFR2-driven cancer cell proliferation. BW710 displays reasonable pharmacokinetic properties with an oral bioavailability of 29 % in mice.

Befotertinib mesylate (D-0316 mesylate) is third-generation tyrosine kinase inhibitor (TKI) of EGFR . It can be used for the research of EGFR T790M-positive non-small cell lung cancer (NSCLC).

Asandeutertinib (Osimertinib-d3, AZD-9291-d3) is an orally administered, ATP-competitive, irreversible, deuterated third-generation Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor (EGFR TKI) and a deuterium-stabilized derivative of osimertinib, with the potential to treat advanced EGFR-mutated NSCLC.

ZJY-54 is an orally active dual-target inhibitor of EGFR/LSD1, with IC50 values of 3.8 nM and 0.6 μM, respectively. ZJY-54 can inhibit the proliferation of non-small cell lung cancer cells, induce the accumulation of H3K4me2 and H3K9me2, and inhibit the phosphorylation of the EGFR signaling pathway. ZJY-54 has anti-tumor activity.

TZEP7 is an EGFR kinase inhibitior in cancer cells. TZEP7 exhibits cytotoxic effects against cancer cell lines and induces apoptosis. TZEP7 demonstrates downregulation of antiapoptotic Bcl-2, upregulation of pro-apoptotic Bax, and increases caspase levels. TZEP7 is promising for research of anticancer agent.

Tyrphostin 63 (compound 13) is an epidermal growth factor receptor (EGFR) inhibitor with IC50 and Ki values are 375 and 123 μM, respectively.

TX2-120-1 possesses the ability to bind to Her3, with an IC50 value of 56 nM for Her3. TX2-120-1 can be used for the synthesis of TX2-121-1, is a TNF-α inhibitor that inhibits endothelial. CC-1069 can be used to study angiogenesis-dependent tumors such as gliomas.

Lazertinib (mesylate) (YH25448 (mesylate); GNS-1480 (mesylate)) is an orally active EGFR inhibitor that can penetrate the blood-brain barrier. Lazertinib (mesylate) inhibits p-EGFR, p-AKT and p-ERK signaling pathways, leading to apoptosis. Lazertinib (mesylate) has anti-tumor activity in the mouse H1975-luc BM xenograft model. Lazertinib (mesylate) can be used in the study of non-small cell lung cancer.

JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC50 of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC50 of 4.9 μM and 0.148 μM, without and with presence of Cetuximab. JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163.

FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a KD value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer.

FRF-06-057 is an ATP-allosteric EGFR inhibitor against wild-type and mutant EGFR, with IC50s of 17 nM (LR/TM), 29 nM (LR/TM/CS), 220 nM (LR), > 1000 nM (WT) respectively.

Emupertinib (example 37) is a potent EGFR inhibitor with IC50 values of <0.3 nM, 0.52 nM, 0.5 nM, 0.69 nM and 0.92 nM for EGFR (d746-750/T790M/C779S), EGFR (L858R/T790M/C797S), EGFR (d746-750/C797S), EGFR (L858R/C797S), and EGFR (wild-type), respectively.

EG31 is an EGFR inhibitor. EG31 effectively inhibits the proliferation of triple-negative breast cancer (TNBC) cells (GI50 values of MDA-MB-231 and Hs578T cells are 498.90 nM and 740.73 nM, respectively) and induces apoptosis by inhibiting the EGFR signaling pathway. EG31 still maintains antiproliferative activity against 5-fluorouracil (5-FU)-resistant TNBC cells (GI50: 519.5 nM). EG31 can be used to study TNBC resistance.

DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models.

CZY43 is a HER3 degrader. CZY43 can effectively induce HER3 degradation in a dose- and time-dependent manner in breast cancer SKBR3 cells. CZY43 potently inhibits HER3-dependent signaling and cancer cell growth and outperforms Bosutinib.