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Src
T2341 KW-2449 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.
T6730 WAY-600 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).
T6732 WYE-687 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).
T2415 PP121 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).
T6886 MCB-613 MCB-613 is an effective steroid receptor coactivator (SRC) stimulator.
T4133 CCT196969 CCT196969 is a novel orally available, pan-RAF inhibitor with anti-SRC activity. It also inhibits SRC, LCK, and the p38 MAPKs.
T2070 CEP-32496 CEP-32496 is a highly potent inhibitor of BRAF.
T2603 CC-292 (AVL-292) Spebrutinib is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.
T6057 URMC-099 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).
T6982 SGI-7079 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.
T6132 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.
T2696 PRT062607 hydrochloride PRT062607 (P505-15, BIIB057) hydrochloride is a novel, highly selective Syk inhibitor.
T4301 AD80 AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.
T6196 PP1 PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
T6266 PP2 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.
T3593 Src I 1 Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor.
T4071 TPX-0005 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.
T1985 WHI-P154 WHI-P154 is a potent JAK3 inhibitor.
T2642 PD173074 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.
T0078 Lapatinib Lapatinib(GW-572016) is an effective ErbB2 and EGFR inhibitor with IC50 of 9.2 and 10.8 nM, respectively.
T2608 CHIR-98014 CHIR-98014 is a selective GSK3 inhibitor; potentiate insulin activation of glucose transport and utilization in vitro and in vivo.
T2327 Pelitinib Pelitinib (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM).
T3063 PD-173955 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.
T1448 Dasatinib Dasatinib Anhydrous is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases.
T6997 SU6656 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.
T6077 ZM 447439 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.
T6078 Saracatinib 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).
T0152 Bosutinib 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.
T1667 Tandutinib 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.
T6235 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.
T6350 CHIR-124 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.
T6896 MLR-1023 MLR-1023 is a chemical compound which inhibits acid secretion in animal models and also acts as a bronchodilator in histamine-challenged animals.
T6419 BMS-536924 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.
T6321 Tofacitinib Tofacitinib is an oral, small molecule inhibitor of Janus kinases that is used to treat moderate-to-severe rheumatoid arthritis.
T1812 KX1-004 KX1-004, a potential protective drug for NIHL, is an effective small molecule inhibitor of Src-PTK.
T3319 Scutellarein Scutellarein reduces inflammatory responses by inhibiting Src kinase activity.
T2398 Tofacitinib citrate Tofacitinib citrate (CP-690550 citrate) is a novel JAK3 inhibitor (IC50: 1 nM), 20- to 100-fold less potent against JAK2/1.
T6680 Staurosporine 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).
T1777 BIBF 1120 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
T1754 ZM 306416 ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
T2325 Neratinib 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
T2610 BMS-599626 BMS-599626 has been used in trials studying the treatment of Cancer, Metastases, and HER2 or EGFR Expressing Advanced Solid Malignancies.
T2624 OSI-930 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.
T2609 Masitinib 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
T2582 Apatinib 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.
T1811 WH-4-023 WH-4-023 is a potent and orally active Lck/Src inhibitor. It also potently inhibits SIK.
T6311 Bafetinib 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.
T1448L Dasatinib monohydrate 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
T6315 MLN8054 MLN8054 is a potent and selective Aurora A kinase inhibitor with an IC50 of 4 nM.
T6345 KX2-391 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
T6227 Benidipine hydrochloride Benidipine HCl, a hydrochloride salt form of benidipine, is used as a blocker of dihydropyridine calcium channel.
T2382 Vemurafenib 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
T2358 ENMD-2076 ENMD-2076, a multi-targeted kinase inhibitor, has specific activity against Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα.
T2709 TAK901 TAK-901 has been used in trials studying the treatment of Lymphoma, Myelofibrosis, Multiple Myeloma, Myeloid Metaplasia, and Advanced Solid Tumors, among others.
T1835 PCI-32765 Ibrutinib is an orally bioavailable, small-molecule inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity.
T6348 NVP-BHG712 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.
T2372 Ponatinib Ponatinib is a tyrosine kinase receptor inhibitor that is used in the therapy of refractory chronic myelogenous leukemia (CML) positive for the Philadelphia chromosome.
T6028 PF-477736 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.
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