tki

ONO-7475 is an inhibitor with high specificity for anexelekto and MER tyrosine kinase

Vorolanib (X-82) is an orally active VEGFR/PDGFR dual inhibitor.

Vodobatinib (K-0706) is a novel 3rd generation (3G) TKI effective against wild-type and mutated BCR-ABL1 with limited off-target activity.

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.

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.

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.

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

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.

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

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.

AKT Kinase Inhibitor is an Akt inhibitor with antitumor activity that selectively inhibits cell proliferation in a dose-dependent manner.

Nimbolide, a triterpenoid derived from neem leaves and flowers, is a natural product and a CDK4/CDK6/NF-κB inhibitor that inhibits multiple signaling pathways including Wnt and PI3K-Akt, possesses antitumor activity, and can induce tumor cell apoptosis.

Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycetes, functioning as an XBP1 inhibitor and inhibiting IRE1α-induced ATP-dependent XBP1 mRNA cleavage (IC50: 80 nM), and induces apoptosis.

Palbociclib (PD 0332991) is a CDK inhibitor that inhibits CDK4 and CDK6 (IC50=11/16 nM) and is orally active. Palbociclib has anti-tumorigenic activity and has investigational potential for use in ER-positive and HER2-negative breast cancer.

Dinaciclib (SCH 727965) is a selective CDK inhibitor targeting CDK1, CDK2, CDK5, and CDK9 (IC50 = 3/1/1/4 nM). It exhibits potential antitumor activity by inhibiting the incorporation of thoracic glycan (dThd) DNA.

RO-3306 is a selectivity ATP-competitive CDK1 inhibitor (Ki: 20 nM). The selectivity of RO-3306 for CDK1 is >15-fold higher than a diverse panel of human kinases.

Abemaciclib (LY2835219) is a dual inhibitor of CDK4/6 (IC50=2/10 nM) with selectivity and specificity. Abemaciclib has antitumor activity and is used to treat advanced or metastatic breast cancer.

Flavopiridol (Alvocidib) (Alvocidib) competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1, 2, 4, 6 versus CDK7. Flavopiridol is initially found to inhibit EGFR and PKA. Phase 1/2.

Monalizumab is a novel immune checkpoint inhibitor targeting natural killer cell population 2A (NKG2A). Monalizumab is a humanized monoclonal antibody against NKG2A that induces IFN-γ production, thereby activating natural killer cell function. Monalizumab has antitumor activity and can be used to study neck squamous cell carcinoma (HNSCC).

Birelentinib (Birelentinib) is an inhibitor of both wild-type and mutant BTK with IC₅₀ values of 6.72 and 6.11 nM, respectively.

5-Iodo-indirubin-3'-monoxime is a potent inhibitor of GSK-3β, CDK5/P25, and CDK1/cyclin B, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20, and 25 nM).

AKT Kinase Inhibitor HCl is an Akt inhibitor with antitumor activity.