c Kit IN 1

c-Kit-IN-1 (DCC-2618) is an effective inhibitor of c-Met and c-Kit (IC50s<200 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].

Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1 4 (IC50: 5 nM ≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.

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.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα β, PDGFR, and Axl.

c-Fms-IN-6 is a potent inhibitor of c-FMS (IC50 ≤10 nM for unphosphorylated c-FMS) and weakly inhibits unphosphorylated c-KIT and PDGFR (IC50: >1 μM).

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).

NAMPT inhibitor-linker 1, a drug-linker conjugate for ADC, integrates an NAMPT inhibitor (as a payload) with a linker. In the formulation of ADC-3, it pairs with an anti-c-Kit monoclonal antibody, demonstrating strong efficacy against c-Kit expressing cell lines, specifically GIST-T1 and NCI-H526, where it exhibits IC50 values of <3 pM and 9 pM, respectively.

C-Kit-IN-6 (Compound 101) is an inhibitor of c-Kit, demonstrating IC50 values ranging from 100 nM to 1 μM.

C-Kit-IN-8 (Compound 53) acts as an inhibitor of c-Kit kinase, hampering uKIT kinase activity with an IC50 greater than 1 μM. Additionally, it inhibits the proliferation of both wild-type and mutant GIST430 and BaF3 cancer cells, exhibiting an IC50 greater than 0.1 μM.

SKLB4771 (FLT3-IN-1) is a novel potent and selective Flt3 inhibitor.

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.

Antitumor agent-70 (compound 8b) is a highly potent multi-targeted kinase inhibitor, particularly targeting c-Kit. It demonstrates remarkable anti-tumor activity and induces cell apoptosis, with strong inhibition of multiple myeloma at an IC50 value of 0.12 μM. Therefore, Antitumor agent-70 holds great potential as an effective therapy for combating cancer, especially in cases involving c-Kit. [1]

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.

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].

Briquilimab (JSP-191), a non-toxic humanized monoclonal antibody, targets CD117 (c-Kit) to deplete hematopoietic stem cells (HSCs), providing a safe approach for clearing host marrow niche to facilitate adequate donor HSC engraftment and immune reconstitution, primarily in the treatment of severe combined immunodeficiency (SCID) [1].

Multi-kinase-IN-6 (compound 10e) is a multikinase inhibitor that impedes the activity of TrkA, ALK2, c-KIT, EGFR, PIM1, CK2α, CHK1, and CDK2. It exhibits antiproliferative effects on MCF7, HCT116, and EKVX cancer cell lines with IC50s of 3.36 μM, 1.40 μM, and 3.49 μM, respectively. Additionally, Multi-kinase-IN-6 induces cell cycle arrest at the G1 S and G1 phases in MCF7 and HCT116 cells, respectively, and effectively triggers apoptosis [1].

Compound 18, also known as FLT3 CHK-IN-1, is a dual inhibitor targeting FLT3 and CHK1, exhibiting over 1700-fold selectivity towards c-KIT and significantly diminishing hERG affinity, with an IC50 of 58.4 μM. It demonstrates efficacy in suppressing tumor growth in mouse xenotransplantation models implanted with MV-4-11 cells [1].

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.

N-Desmethyl Regorafenib N-oxide, an active metabolite of the multi-kinase inhibitor regorafenib, originates through the action of the cytochrome P450 (CYP) isoform CYP3A4. This compound demonstrates efficacy in vitro by inhibiting key enzymes such as VEGFR2, Tie2, c-Kit, and B-RAF, and it exhibits tumor growth inhibition in HT-29 and MDA-MB-231 mouse xenograft models at a dosage of 1 mg/kg.

Apatinib-d8 is a deuterated compound of Apatinib. Apatinib has a CAS number of 811803-05-1. Apatinib is an orally bioavailable and specific VEGFR2 inhibitor (IC50: 1 nM). In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.