tki

Tarlox-TKI (Kinase inhibitor-1) is a pan-ErbB inhibitor, the active ingredient of Tarloxotinib, with antitumor activity.Tarlox-TKI inhibits NRG1 and suppresses HER2 mutants.

TKIM is a TWIK-related potassium channel 1 (TREK-1) inhibitor, binding to the pocket of the intermediate (IM) state of TREK-1.

Vabametkib, a potent hepatocyte growth factor receptor (HGFR) inhibitor, exhibits anti-proliferative effects on Hs746T cells and selectively inhibits c-Met with an IC50 value of 7 nM, showcasing its potential as an antineoplastic agent.

Tkip is a specific inhibitor of JAK2. It binds to the autophosphorylation site of JAK2, thereby inhibiting JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1. Tkip can suppress the antiviral activity of IFN-γ and the expression of MHC class I molecules. Tkip is applicable in studies related to the IFN-γ signaling pathway.

BI-4732 is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) with high blood-brain barrier permeability, antitumor activity, inhibition of EGFR activation, and inhibition of T790M mutations.

Nilotinib monohydrochloride monohydrate (Nilotinib (monohydrochloride monohydrate)) is significantly potent BCR-ABL against, is a second generation tyrosine kinase inhibitor (TKI), and is active against many BCR-ABL mutants.

NT157 is a small molecule tyrphostin targeting IRS protein and has the potential to inhibit IGF-1R and STAT3 signaling pathways in TME cancer cells and stromal cells, resulting in decreased cancer cell survival.

EGFR-IN-8, a dual inhibitor targeting both EGFR and c-Met, shows potential as a promising candidate for further development in treating EGFR TKI-resistant NSCLC.

MRX-2843 (UNC2371) is a potent and orally active inhibitor of MERTK and FLT3(IC50s of 1.3 nM and 0.64 nM, respectively).

Boc-C5-O-C5-O-C6-Cl (PROTAC Linker 2) is a chemical compound primarily used as a linker in PROTAC applications, facilitating the connection between a specific tyrosine kinase inhibitor (TKI) and the E3 recruiting ligand.

HG-6-63-01 serves as a type II RET tyrosine kinase inhibitor (TKI). It effectively targets and inhibits REarranged during Transfection (RET) kinase, disrupting signaling pathways in human thyroid cancer cell lines possessing oncogenic RET alleles. Moreover, this compound reduces the phosphorylation and signaling of RET oncogenic mutants. HG-6-63-01 further suppresses the proliferation of fibroblasts transformed by RET C634R and RET M918T, as well as thyroid cancer cells with RET mutations, showing potential as a therapeutic option for cancers with oncogenic activation of RET.

Mavelertinib (PF-06747775) is an orally available, selective and potent EGFR tyrosine kinase (EGFR TKI) inhibitor with inhibitory effects on T790M L858R and T790M Del, and can be used in the study of oncology and respiratory diseases.

Transtinib is an effective and irreversible EGFR tyrosine kinase inhibitor (EGFR-TKI) that is active against L858R/T790M mutated NSCLC cell lines and xenografts.

Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19 T790M, L858R T790M, Del19, L85R and Wild type EGFR respectively.

Oritinib (SH-1028) is an inhibitor of EGFR with IC50s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM for EGFR (wt), EGFR (L858R), EGFR (L861Q), EGFR (L858R T790M), EGFR (d746-750), EGFR (d746-750 T790M), respectively. Oritinib can be used in studies about the treatment of non-small cell lung cancer.

AKN-028 acetate, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. It inhibits FLT3 autophosphorylation and induces a dose-dependent cytotoxic response (mean IC50 = 1 μM). AKN-028 acetate also induces apoptosis by activation of caspase 3 and can be used in acute myeloid leukemia (AML) research [1].

Dovitinib Dilactic Acid (Dovitinib (TKI-258) Dilactic Acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3 c-Kit) with IC50 of 1 nM 2 nM, also potent to class IV (FGFR1 3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

Epitinib is an orally active, selective, blood-brain barrier crossing epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI).

Dovitinib is an orally active, multi-targeted tyrosine kinase (RTK) inhibitor with anti-tumor effects.

JBJ-09-063 is a mutant-selective allosteric inhibitor of the epidermal growth factor receptor (EGFR), with potent inhibitory activity demonstrated by half-maximal inhibitory concentrations (IC50s) of 0.147 nM for EGFR L858R, 0.063 nM for EGFR L858R T790M, 0.083 nM for EGFR L858R T790M C797S, and 0.396 nM for EGFR L747S. This compound effectively decreases phosphorylation of EGFR, Akt, and ERK1 2, showing efficacy in both EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 holds potential for research into EGFR-mutant lung cancer.

Dovitinib lactate hydrate (TKI258) is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3 c-Kit) with IC50 of 1 nM 2 nM, also potent to class IV (FGFR1 3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

CEP-11981 is an orally active TIE2 pan-VEGFR inhibitor with broad tyrosine kinase inhibitory activity, exhibiting antitumour and anti-angiogenic effects, and is applicable for the treatment of refractory solid tumours.

Dovitinib lactate (TKI-258 lactate)(TKI258) lactate is a potent inhibitor of fibroblast growth factor receptor 3 (FGFR3) (IC50 :5 nM).

Larotinib mesylate hydrate is a potent, broad-spectrum, and orally active tyrosine kinase inhibitor (TKI), primarily targeting EGFR with an IC50 value of 0.6 nM.