c-kit

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.

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 Antibody (LMJ729) is a humanized monoclonal antibody expressed in CHO cells that targets SCFR/c-Kit/CD117. While the antibody itself has limited inhibitory effects on cell proliferation, Anti-c-Kit Antibody (LMJ729) can serve as a targeted carrier for antibody-drug conjugates, facilitating the delivery of cytotoxic molecules and exerting antitumor activity.

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.

c-Kit-IN-7 (compound 104) serves as an effective inhibitor of c-Kit, exhibiting an IC50 of 10 nM or less. It plays a crucial role in cancer research.

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.

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-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-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-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.

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

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.

Sorafenib (Bay 43-9006) is a multikinase inhibitor that targets Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. It exhibits antitumor properties and can induce autophagy, apoptosis, and agonistic iron death.

Lenvatinib (E7080) is a multi-target receptor tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, KIT, PDGFR, and RET, and has oral activity. Lenvatinib has the strongest inhibitory activity on VEGFR2 and VEGFR3 (IC50=4/5.2 nM). Lenvatinib has strong anti-tumor activity.

Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma.

Imatinib Mesylate (STI-571) is a tyrosine kinase receptor inhibitor with antineoplastic activity (IC50s: 0.6 μM, 0.1 μM and 0.1 μM for v-Abl, c-Kit and PDGFR, respectively).

Pexidartinib (PLX-3397) is a capsule containing a small-molecule receptor tyrosine kinase (RTK) inhibitor targeting KIT, CSF1R, and FLT3, with potential antineoplastic activity.

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.

Gilteritinib (ASP2215) is a potent inhibitor of FMS-related tyrosine kinase 3 (FLT3) and AXL tyrosine kinase receptors (IC50 = 0.29 nM and <1 nM, respectively). In preclinical studies, gilteritinib demonstrated strong antileukemic and antitumor effects. Gilteritinib is currently in several Phase 3 clinical trials for acute myeloid leukemia.

Avapritinib (BLU-285) is a selective, highly potent, and orally active inhibitor of KIT and PDGFRA activation loop mutant kinases, targeting KIT D816V (IC50:0.27 nM) and PDGFRA D842V (IC50:0.24 nM), and attenuates the transport functions of ABCB1 and ABCG2. It binds to the active conformation of the kinases and exhibits antitumor activity.

Ripretinib (DCC-2618) is an orally bioavailable inhibitor of (KIT) and (PDGFRA).

SU11652 is an effective and competitive receptor tyrosine kinase (RTK) inhibitor, including VEGFR, FGFR, PDGFR, and Kit. SU11652 disrupts the function of all forms of mutant Kit and may be used in the study of cancers involving Kit mutations.