c Kit IN 2

c-Kit-IN-2 is a c-KIT inhibitor (IC50: 82 nM) exhibiting superior antiproliferative activities against all three GIST cell lines, GIST430, GIST882, and GIST48 (GI50s: 1, 3, and 2 nM).

JNK-IN-8 (JNK Inhibitor XVI) is an irreversible JNK1 2 4 inhibitor (IC50: 4.7 18.7 1 nM) with over 10-fold selectivity compared to MNK2 and Fms, and no inhibition of Met, c-Kit, or PDGFRβ in the A375 cell line.

Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

AMG-25 (c-Kit-IN-5-1) is a selective and potent c-Kit inhibitor that inhibits c-Kit, KDR, p38, Lck, and Src, and can be used in the study of mast cell-associated fibrosis.

PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.

Pyridostatin Trifluoroacetate Salt is a G-quadruplexe stabilizer with Kd of 490 nM in a cell-free assay, which targets a series of proto-oncogenes including c-kit, K-ras and Bcl-2.

Henatinib is an orally active small molecule multi-kinase inhibitor with broad antitumour effects. henatinib inhibits the activity of VEGFR-2 (IC50: 0.6 nM), c-kit (IC50: 3.3 nM), PDGFR (IC50: 41.5 nM). henatinib significantly inhibits VEGFR-2 phosphorylation and its downstream signalling pathways in human umbilical vein endothelial cells (HUVECs). Henatinib significantly inhibited VEGFR-2 phosphorylation and its downstream signaling pathway in human umbilical vein endothelial cells (HUVECs).

Multi-kinase-IN-2 is an orally active inhibitor of angiokinases. multi-kinase-IN-2 significantly inhibits the activity of angiokinases such as VEGFR-1 2 3, PDGFRα β, FGFR-1, LYN and c-KIT kinases. -IN-2 significantly attenuates phosphorylation of AKT and ERK proteins, induces apoptosis and has anticancer effects.

Famitinib malate (SHR1020) is an orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively. It induces cell apoptosis and demonstrates potent antitumor activity in human gastric cancer cells and xenografts, making it a valuable compound for cancer research.

Apatinib, also known as Rivoceranib and YN-968D1, is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. The free-base form is also known as Rivoceranib. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.

Imatinib Impurity E is a specific impurity found in Imatinib, an orally available inhibitor of multiple tyrosine kinases, including BCR ABL, v-Abl, PDGFR, and c-kit. Imatinib (STI571) operates by semi-competitively inhibiting enzyme activity; it binds adjacent to the ATP binding site, inducing a closed or self-inhibited conformation [1] [2] [3] [4]. Additionally, Imatinib acts as an inhibitor against SARS-CoV and MERS-CoV [5].

FAK-IN-14 is a highly effective focal adhesion kinase (FAK) inhibitor that induces apoptosis and cell cycle arrest. FAK-IN-14 has weak inhibitory effects on Akt, c-kit, MEK1 2 and mTOR, but has significant inhibitory effects on FAK, FGFR1 and Pyk2.

CYY292 is a chemical compound acting as an inhibitor of PDGFRα, PDGFRβ, FGFR1, -2, and -3, with respective IC50 values of 5.35, 4.6, 28, 28, and 78 nM. It exhibits selectivity over FGFR4 (IC50 > 1,000 nM) while also targeting c-Kit, VEGFR2, VEGFR1, and IGF-1R (IC50 values of 67, 33, 36, and 75 nM, respectively). Additionally, CYY292 inhibits EGFR, BTK, Cdk4/cyclin D3, and MET with IC50 values of 128, 198, 214, and 396 nM, respectively. This compound demonstrates efficacy in arresting the proliferation of various osteosarcoma cell lines—MG-63, U2OS, MNNG/HOS, and Saos-2—with IC50s ranging from 0.72 to 1.36 µM. Moreover, CYY292 at 0.3 and 0.5 µM concentrations inhibits migration and invasion in glioblastoma cells (U87MG and LN-229) and, at a dose of 30 mg/kg, decreases tumor volume and enhances survival in a U87MG orthotopic mouse xenograft model.