BT5528 is a bicyclic peptide toxin conjugate, an EphA2 activator. BT5528, made up of a bicyclic peptide and Auristatin E (HY-15582), is derivated from BCY6099. BT5528 shows potent anti-tumor activity without bleeding or coagulation toxicity in rats model[1][2].
JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis[1].
Hypothemycin, a fungal polyketide, is a multikinase inhibitor with Kis of 10/70 nM, 17/38 nM, 90 nM, 900 nM/1.5 μM, and 8.4/2.4 μM for VEGFR2/VEGFR1, MEK1/MEK2, FLT-3, PDGFRβ/PDGFRα, and ERK1/ERK2, respectively[1][2].
Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871[1].
Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively[1].
Leucettinib-92 (compound 92) is an inhibitor of DYRK/CLK kinase, The IC50s are 147 nM (CLK1), 39 nM (CLK2), 5.2 nM (CLK4), 0.8 μM (CLK3), 124 nM (DYRK1A), 204 nM (DYRK1B), 0.16 μM (DYRK2), respectively. 1.0 μM (DYRK3), 0.52 μM (DYRK4), 2.78 μM (GSK3)[1].
Lck Inhibitor is a new class of compounds that are potent inhibitors of Lck with an IC50 value of 7 nM.IC50 Value: 7 nM [1]Target: Lckin vitro: Lck Inhibitor (compound 25) exhibited good potency in the T-cell receptor-induced IL-2 secretion assay (IL- 2) and also inhibited subsequent T-cell proliferation (T-cell prolif.) in the same human T -cells.in vivo: A once daily dose of 25was administered orally at 10, 30, and 60 mg/kg from day 9 today 17. Paw volume was measured daily from day 9 through day 18. The compound showed a dose-dependent inhibition of arthritis, with an ED50 estimated at 24 mg/kg (Figure 6). Based on the measured plasma levels from the three dose groups, the exposure of 25 at the ED50 was estimated to be 2.7 μM·h (Cmax≈ 0.7 μM) [1].Clinical trial: N/A
CPD-1224 is an orally active derivative of ALK inhibitors to cereblon ligands. CPD-1224 targets to EML4-ALK oncogenic fusions, and degrades ALK and mutant L1196M/G1202R[1].
BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC50 of ≤100 nM for Ba/F3Bcr-AblT3151. BCR-ABL-IN-3 has anti-cancer activity[1].
AnnH31 is a potent Inhibitor of DYRK1A Kinase.
Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of MET tyrosine kinase with a dissociation constant (Ki) of 2 nM.
PROTAC IRAK4 degrader-5 is a PROTAC-based IRAK4 degrader extracted from patent US20190192668A1, compound I-171[1].
BLZ945 is a potent, selective and brain-penetrant CSF-1R inhibitor with an IC50 of 1 nM, showing more than 1,000-fold selectivity against its closest receptor tyrosine kinase homologs.
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities[1].
Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative isolated from plants of the Genus Daphne, is a protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively[1][2]. Daphnetin (7,8-dihydroxycoumarin) is a secondary metabolite of plants used in folk medicine to counter inflammatory and allergic diseases, also has been clinically used in the treatment of coagulation disorders, rheumatoid arthritis with anti-malarian and anti-pyretic properties[3].
TIE-2/VEGFR-2 kinase-IN-2 is a potent dual VEGFR2 and Tie-2 inhibitor with pIC50 values of 8.61 and 8.56, respectively[1]. TIE-2/VEGFR-2 kinase-IN-2 is an anti-angiogenic agent and can be used for cancer research[2].
GNF4877 is a potent DYRK1A and GSK3β inhibitor with IC50s of 6 nM and 16 nM, respectively, which leads to blockade of nuclear factor of activated T-cells (NFATc) nuclear export and increased β-cell proliferation (EC50 of 0.66 μM for mouse β (R7T1) cells)[1].
Ripretinib (DCC-2618) is a pan-KIT and PDGFRA inhibitor, and has antitumor activity.
Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].
Dosimertinib is a highly potent, selective, and orally efficacious deuterated EGFR targeting clinical candidate for the treatment of non-small-cell lung cancer.
EGFR/HER2-IN-3 (Compound ZINC21942954) is a dual inhibitor of EGFR and HER2[1].
WY-135 is a ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
Bucladesine calcium salt(DC2797 calcium salt) is a membrane permeable selective activator of PKA.Target: PKABucladesine (bilateral infusion of 10 mM or 100 mM) leads to a significant reduction in escape latency and travel distance (showing an improvement in spatial memory) compared to the control, as assesed by Morris water maze task in male rats. Bucladesine at 1 mM and 5 mM concentrations infused within minutes after 0.5 mg nicotine infusion improves spatial memory retention in male rats [1]. Bucladesine (10 mM/side) combined with Nicotine (0.5 mM/side) results in a significant increase in the ChAT and VAChT immunoreactivity in CA1 regions, and increase in the optical density and amount of ChAT and VAChT immunostaining correlates with the decrease in escape latency and traveled distance in rats treated with Nicotine and low dose of Bucladesine [2]. Bucladesine is absorbed very rapidly and almost completely when the aqueous solution is applied to the site where the skin has been excised. Bucladesine is absorbed rapidly but slower than in the full-thickness abrasion rat model in the case of stripped skin [3]. Bucladesine (single or multiple administration of an emulsion containing 1.5%) is capable of significantly reducing the inflammatory oedema in the arachidonic acid induced ear oedema model in mice [4].
Regorafenib (BAY 73-4506) mesylate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib mesylate shows very robust antitumor and antiangiogenic activity[1].
FAK-IN-5 (Compound 8l) is a FAK signaling inhibitor. FAK-IN-5 induces cell apoptosis and autophagy[1].
Gefitinib N-oxide is the N-oxide derivative of Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells[1][2].
JAK3/BTK-IN-1 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-1 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 002)[1].
c-Fms-IN-13 (compound 14) is a potent FMS kinase inhibitor with an IC50 value of 17 nM. c-Fms-IN-13 can be used as an anti-inflammatory agent[1].
AD57 is an orally active multikinase inhibitor, inhibits RET, BRAF, S6K and Src, with greatly reduces mTOR activity[1].
EGFR-IN-21 is a potent EGFR inhibtior with an IC50 of 0.38 nM. EGFR-IN-21 has antitumor activity[1].