||KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 (IC50: 6.6 nM), modestly effective to Bcr-Abl, FGFR1, and Aurora A; little inhibitory on PDGFRβ, IGF-1R, EGFR.
||WAY-600 is a potent, ATP-competitive and selective inhibitor of mTOR with IC50 of 9 nM; blocks mTORC1/P-S6K(T389) and mTORC2/P-AKT(S473) but not P-AKT(T308); selective for mTOR than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
||WYE-687 is an ATP-competitive and selective inhibitor of mTOR with IC50 of 7 nM; blocks mTORC1/pS6K(T389) and mTORC2/P-AKT(S473) but no effect observed on P-AKT(T308). Selectivity for mTOR is greater than PI3Kα (>100-fold) and PI3Kγ (>500-fold).
||PP-121 is a multi-targeted inhibitor of PDGFR (IC50: 2 nM), Hck (IC50: 8 nM), mTOR (IC50: 10 nM), VEGFR2(IC50: 12 nM), Src (IC50: 14 nM) and Abl (IC50: 18 nM) , also inhibits DNA-PK (IC50: 60 nM).
||MCB-613 is an effective steroid receptor coactivator (SRC) stimulator.
||CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
||CEP-32496 is a highly potent inhibitor of BRAF.
||Spebrutinib is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.
||URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).
||SGI-7079 is a new selective Axl inhibitor. SGI-7079 can be a dose-dependent manner inhibited growth of tumors. It is also a potential therapeutic target for EGFR inhibitor resistance.
||ENMD-2076 L-(+)-Tartaric acid
||ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.
||PRT062607 (P505-15, BIIB057) hydrochloride is a novel, highly selective Syk inhibitor.
||AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
||PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
||PP2 is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
||Src I 1
||Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor.
||TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.
||WHI-P154 is a potent JAK3 inhibitor.
||PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.
||Lapatinib(GW-572016) is an effective ErbB2 and EGFR inhibitor with IC50 of 9.2 and 10.8 nM, respectively.
||CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
||Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
||PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.
||Dasatinib Anhydrous is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases.
||SU 6656 is a selective inhibitor of Src family kinases, with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.
||ZM 447439 is a selective and ATP-competitive inhibitor for Aurora A and Aurora B with IC50 of 110 nM and 130 nM, respectively. It is more than 8-fold selective for Aurora A/B than MEK1, Src, Lck and has little effect against CDK1/2/4, Plk1, Chk1, etc.
||Saracatinib (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to c-Yes, Lyn, Fyn, Fgr, Blk and Lck; less active for Abl and EGFR (L858R and L861Q).
||Bosutinib is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Bosutinib inhibits the autophosphorylation of both Abl and Src kinases, resulting in inhibition of cell growth and apoptosis.
||Tandutinib (MLN518, CT53518), an effective FLT3 antagonist (IC50: 0.22 μM), can also inhibit c-Kit and PDGFR, 15-20 fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR, and KDR.
||Lapatinib (GW-572016) Ditosylate
||Lapatinib Ditosylate, an effective EGFR and ErbB2 inhibitor, is with IC50 of 10.8 and 9.2 nM for EGFR and ErbB2, respectively.
||CHIR-124 is an effective Chk1 inhibitor (IC50: 0.3 nM). It has 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against Cdc2 and CDK2/4.
||MLR-1023 is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals.
||BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.
||Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
||KX1-004, a potential protective drug for NIHL, is an effective small molecule inhibitor of Src-PTK.
||Scutellarein reduces inflammatory responses by inhibiting Src kinase activity.
||Tofacitinib citrate (CP-690550 citrate) is a novel JAK3 inhibitor (IC50: 1 nM), 20- to 100-fold less potent against JAK2/1.
||Staurosporine is a potent PKC inhibitor for PKCα/γ/η (IC50: 2/5/4 nM), less potent to PKCε (73 nM), PKCδ (20 nM) and little action to PKCζ (1086 nM).
||Nintedanib is an orally bioavailable, indolinone-derived, receptor tyrosine kinase (RTK) inhibitor (VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM) with potential antiangiogenic and antineoplastic activities. Multitargeted tyrosine kinase inhi
||ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
||Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor (IC50: 59/92 nM) for HER2 and EGFR, respectively. Neratinib binds to the HER-2 receptor irreversibly, thereby reducing autophosphorylation in cells, apparently by targeting a cysteine residue in the ATP-binding pocke
||BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
||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.
||Masitinib is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distrib
||Apatinib is an orally bioavailable and specific VEGFR2 inhibitor (IC50: 1 nM). In addition, this agent mildly inhibits c-Kit and c-SRC tyrosine kinases.
||WH-4-023 is a potent and orally active Lck/Src inhibitor. It also potently inhibits SIK.
||Bafetinib (INNO-406) is an effective and specific dual Bcr-Abl/Lyn inhibitor (IC50: 5.8/19 nM), and no inhibition of the phosphorylation of the T315I mutant and less effective to c-Kit and PDGFR.
||Dasatinib is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently, because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown
||MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.
||KX2-391 is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-clinical animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibitor. KX2-391, belongs to an emerging new family of targeted cancer treatments called protein kinas
||Benidipine HCl, a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.
||Vemurafenib (PLX4032, RG7204) is a novel and potent B-RafV600E inhibitor (IC50 of 31 nM, in the cell-free assay). Vemurafenib selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downs
||ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
||TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
||Ibrutinib is an orally bioavailable, small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
||NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
||Ponatinib is a tyrosine kinase receptor inhibitor that is used in the therapy of refractory chronic myelogenous leukemia (CML) positive for the Philadelphia chromosome.
||PF-477736 is a specifc, effective and ATP-competitive Chk1 inhibitor (Ki: 0.49 nM ) and also inhibits FGFR3, Aurora-A, VEGFR2, Flt3, Fms (CSF1R), Ret and Yes.