c kit in 1

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

c-KitReceptor modulator-1 (Compound #22) is a regulator of the c-Kit receptor. This compound is applicable in research focused on malignant cancers such as canine mast cell tumors, human gastrointestinal stromal tumors, and small cell lung cancer.

Anti-c-Kit/CD117 Antibody (SR-1) is a mouse IgG2a, κ chimeric antibody that specifically targets human c-Kit/CD117. The recommended isotype control for this antibody is Mouse IgG2a kappa, Isotype Control.

c-Kit-IN-10 (Compound 1) is an inhibitor of c-Kit. It is useful in research related to inflammation and malignant cancers, such as asthma.

c-Kit-IN-14 (Compound 1) is a c-kit kinase inhibitor. It effectively inhibits the phosphorylation of wild-type c-kit, with an IC50 value of 0.4 nM for pKIT. Additionally, c-Kit-IN-14 inhibits Exon 11 KIT with an IC50 value of 0.4 nM. This compound is applicable in the research of mast cell-mediated diseases, such as urticaria.

c-Kit-IN-11 (Compound A7) is a c-Kit inhibitor with an IC50 of 76 nM against Mo7e cells. This compound is applicable for research in inflammatory conditions like asthma and malignant cancers.

c-Kit-IN-12 (Compound 2a) is a potent c-Kit inhibitor with an IC50 of less than 10 nM across four KIT mutant cell models [BAF3 KIT EX11 DEL, EX11 DEL/D816H, EX11 DEL/T670I, EX11 DEL/V654A]. It is useful for research into c-Kit-associated diseases or disorders, such as cancer.

c-Kit-IN-13 (Compound I) is an inhibitor of the c-kit kinase. It suppresses the autophosphorylation of the wild-type c-kit, with an IC50 of 0.3 nM for pKIT. Additionally, c-Kit-IN-13 inhibits Exon 11 KIT with an IC50 of 0.9 nM. This compound can be utilized in research on mast cell-mediated diseases such as urticaria.

(S)-c-Kit-IN-12 (Compound 2b) is a potent c-Kit inhibitor with an IC50 of less than 10 nM against four KIT mutant cell models [BAF3 KIT EX11 DEL, EX11 DEL/D816H, EX11 DEL/T670I, EX11 DEL/V654A]. This compound is useful for researching diseases or disorders related to c-Kit, such as cancer.

JNK-IN-8 (JNK Inhibitor XVI) is an effective JNK inhibitor that inhibits JNK1, JNK2, and JNK3 with IC₅₀ values of 4.7, 18.7, and 1 nM, respectively. JNK-IN-8 offers the advantages of minimal off-target activity, sustained inhibition, and high specificity. JNK-IN-8 primarily acts by blocking the JNK/c-Jun signaling pathway, inhibiting the phosphorylation of the downstream transcription factor c-Jun, thereby regulating the expression of genes associated with inflammatory responses, apoptosis, and stress responses. JNK-IN-8 can be used in research on tumors, inflammation, and neurological diseases.

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.

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-targeted inhibitor with an IC₅₀ of 82 nM. It exhibits favorable anti-proliferative effects on three gastrointestinal stromal tumor cell lines GIST882, GIST430, and GIST48, with corresponding GI₅₀ values of 3 nM, 1 nM, and 2 nM, respectively.

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.

c-Kit-IN-9 (Compound D9) is an inhibitor of c-Kit. It suppresses inflammation in J774A.1, RAW264.7, MPMs cells, and lung tissue by blocking LPS-induced NF-κB pathway activation. Additionally, c-Kit-IN-9 demonstrates effective anti-inflammatory activity in mouse models of acute lung injury and sepsis. It is useful for research on acute lung injury and related inflammatory diseases.

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.

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.

Midostaurin (PKC412) is a multi-targeted tyrosine kinase inhibitor with antitumor activity, exhibiting IC50 values ranging from 22 to 500 nM against PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ, and VEGFR1/2. Midostaurin is indicated for the treatment of acute myeloid leukemia (AML) and systemic mastocytosis (SM).

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

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]