Dual DDR1 and DDR2 inhibitor 5n is a highly potent and selective small molecule inhibitor targeting both Discoidin Domain Receptor 1 (DDR1) and Discoidin Domain Receptor 2 (DDR2). These receptors are receptor tyrosine kinases (RTKs) that play critical roles in cell proliferation, migration, and extracellular matrix (ECM) remodeling. Dysregulation of DDR1 and DDR2 has been implicated in various diseases, including cancer, fibrosis, and inflammation, making them attractive therapeutic targets.

ATH686 (ATH-686) is a potent and selective, second-generation inhibitor of mutant FLT3 protein kinase.

Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy.

Allitinib (AST-1306, ALS1306)) is a novel potent, selective irreversible EGFR and HER2 inhibitor with IC50 of 0.5 and 3 nM in cell-free assays.

TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.

Lanraplenib monosuccinate (GS-9876 monosuccinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib monosuccinate (GS-9876 monosuccinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.

RU-302 is a small molecule pan-TAM inhibitor that targets the TAM Ig1-Gas6 interface, blocks Gas6-dependent TAM activation.

GSK-626616 is a dual-specificity tyrosine-regulated kinase (DYRK3) inhibitor with an IC50 of 0.7 nM which is a potential therapy for the treatment of anemia.

MAX-40279 hemifumarate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemifumarate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032).

MAX-40279 hemiadipate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemiadipate has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032).

MAX-40279 is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 has the potential for the research of acute myelogenous leukemia (AML) (extracted from patent WO2021180032).

Src kinase inhibitor I is a potent competitive inhibitor of both Src and Lck (IC50 = 44 and 88 nM, respectively), as well as Csk and Yes.

Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q).

Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 0.21 nM/0.16 nM/0.24 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met EGFR and IGF-1R.

Tivozanib hydrochloride hydrate is a potent and selective and orally active VEGFR tyrosine kinase inhibitor with IC50是of 0.21, 0.16, 0.24 nM for VEGFR-1, VEGFR-2, VEGFR-3, respectively. Tivozanib hydrochloride hydrate inhibits angiogenesis and vascular permeability in tumor tissues and shows antitumor activity. Tivozanib hydrochloride hydrate has the potential for the research of metastatic renal cell carcinoma (RCC) .

A novel protein kinase affinity probe...

E-7050 is hepatocyte growth factor receptors (HGFR).

KX2-391, the first clinical Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

SU14813 is an oral, multitargeted tyrosine kinase inhibitor (TKI) targeting vascular endothelial growth factor receptors (VEGFR), platelet-derived growth factor receptors (PDGFR), Kit, and fms-like tyrosine kinase 3 (FLT-3).

BMS-986195 is a potent, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK).

NRPa-308 is a neuropilin-1 (NRP-1) antagonist, inhibits the VEGF-A165/NRP-1 binding with IC50 of 42 uM, exerts in vitro anti-angiogenic activity.

GZD824 dimesylate (HQP1351 dimesylate) is an orally bioavailable pan-Bcr-Abl inhibitor with potency against a wide range of Bcr-Abl mutants and the native enzyme (IC50=0.34 nM). GZD824 dimesylate has antitumor activity.

DYRK2 inhibitor C17 is a potent, selective DYRK2 inhibitor with IC50 of 9 nM, weakly inhibits DYRK3 (IC50=68 nM), and does not inhibit DYRK1A/1B (IC50>2000 nM).C17 showed outstanding selectivity for the human kinome containing 467 other human kinases.C17 showed synergistic 4E-BP1 phosphorylation suppression combined with AKT and MEK inhibitors.C17 impeded the store-operated calcium entry process (ORAI1 channel).

WM-S1-030 is a highly potent, specific inhibitor of recepteur d'origine nantais (RON kinase, MST1R) with IC50 of 0.39 nM in in vitro enzyme activity.

EGFR-IN-99 (compound 1a) is a potent EGFR and HER2 Exon 20 insertion mutant inhibitor. EGFR-IN-99 has excellent antiproliferative activity against DFCI127 cells, with an EC50 of 11.5 nM. EGFR-IN-99 can be used for the research of non-small cell lung cancer (NSCLC).

OBX02-011 is a potent, reversible, fourth-generation EGFR tyrosine kinase inhibitor (TKI) that overcomes the EGFR C797S mutation, inhibits triple mutants Del19/T790M/C797S and L858R/T790M/C797S with IC50 of 0.134 and 2.09 nM, respectively.

Ansornitinib is an orally active dual kinase inhibitor that inhibits platelet-derived growth factor receptor (PDGFR) and vascular endothelial growth factor receptor (VEGFR2). Ansornitinib can be used as an antifibrotic agent in lung, liver, kidney, and gastrointestinal fibrotic diseases.

Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities.

EGFR/ErbB-2/ErbB-4 inhibitor-2 (Compound 5) is a EGFR and ErbB inhibitor with IC50s of 0.017 μM, 0.08 μM, 1.91 μM.

WAY-340935 (VEGFR2-IN-2) can inhibit the function of VEGFR2 and the anti-proliferative activity against the H460 cell line is produced partly by interaction of VEGFR protein.