首页 > Autophagy > Bcr-Abl
Bcr-Abl
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.
T0186 Docetaxel trihydrate Docetaxel is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumor including breast and lung cancer. Therapy with docetaxel has been associated with a low rate of serum enzyme eleva
T0448 (S)-(+)-Ibuprofen Dexibuprofen, S(+)-ibuprofen, is a non-steroidal anti-inflammatory drug (NSAID), inhibiting cyclooxygenase (COX).
T1034 Docetaxel Docetaxel, a microtubule inhibitor, binds specifically to the beta-tubulin subunit of microtubules and thereby antagonizes the disassembly of the microtubule proteins.
T1119 Rasagiline Rasagiline is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinsons disease.
T1448 Dasatinib Dasatinib Anhydrous is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases.
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
T1493 BH3I-1 BH3I-1 is a Bcl-2 antagonist.
T1524 Nilotinib Nilotinib is an orally bioavailable aminopyrimidine-derivative Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. Designed to overcome imatinib resistance, nilotinib binds to and stabilizes the inactive conformation of the kinase domain of the Abl protein of the Bcr-Abl fusion protein,
T1621 Imatinib Mesylate Imatinib mesylate is a specific tyrosine kinase receptor inhibitor with antineoplastic activity, used in the therapy of Philadelphia chromosome-positive chronic myelogenous leukemia and gastrointestinal stromal tumors.
T1754 ZM 306416 ZM 306416, a VEGFR1 inhibitor (IC50: 0.33 μM), can also inhibit EGFR (IC50<10 nM).
T1803 GNF-5 GNF-5 is a specific non-ATP competitive inhibitor of Bcr-Abl (IC50: 0.22±0.1 uM, Wild-type Abl). It is an analog of GNF-2 with improved pharmacokinetic properties.
T1817 GNF-2 GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.
T1980 HA14-1 HA14-1, a Bcl-2/Bcl-XL antagonist, is a non-peptidic ligand of a Bcl-2 surface pocket (IC50: ~9 μM).
T2070 CEP-32496 CEP-32496 is a highly potent inhibitor of BRAF.
T2094 Danusertib Danusertib is a small-molecule 3-aminopyrazole derivative with potential antineoplastic activity. Danusertib binds to and inhibits the Aurora kinases, which may result in cell growth arrest and apoptosis in tumor cells in which Aurora kinases are overexpressed.
T2099 ABT-737 BH3 Mimetic ABT-737 is an orally bioavailable, selective small molecule B-cell lymphoma 2 (Bcl-2) Homology 3 (BH3) mimetic, with potential pro-apoptotic and antineoplastic activities.
T2101 Navitoclax Navitoclax is an orally active, synthetic small molecule and an antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity.
T2116 AEE788 AEE788 has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
T2119 ABT-199 (GDC-0199) Venetoclax is an orally bioavailable, selective small molecule inhibitor of the anti-apoptotic protein Bcl-2, with potential antineoplastic activity.
T2293 SGX-523 SGX-523 is a selective Met inhibitor (IC50: 4 nM), no inhibitory to Abl, BRAFV599E, p38α, and c-Raf.
T2328 Radotinib Radotinib, and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of Y, most notably Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) with resistance or intolerance of other tyrosine kinase Bcr-Abl inhibitors
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.
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.
T2429 GZD824 Dimesylate GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I).
T2509 Tozasertib VX-680 (Tozasertib, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A (Kiapp: 0.6 nM) in a cell-free assay, less effective towards Aurora B/C and 100-fold more selective for Aurora A than 55 other kinases.
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
T2640 DCC-2036 (Rebastinib) DCC-2036 (Rebastinib) is a conformational control Bcr-Abl inhibitor for Abl1(WT, IC50: 0.8 nM) and Abl1(T315I, IC50: 4 nM), also inhibits LYN, SRC, HCK, FGR, FLT3, KDR, and Tie-2, and low activity to c-Kit.
T2730 Gossypol acetic acid Gossypol-acetic acid, a polyphenolic compound isolated from cottonseeds, binds with Bcl-2, Bcl-xL, Mcl-1, and does not inhibit BIR3 domain and BID.
T2802 Nocodazole Nocodazole is a synthetic inhibitor of microtubule polymerization, also inhibits Abl (IC50: 0.21 μM), Abl(E255K, IC50: 0.53 μM) and Abl(T315I, IC50: 0.64 μM) in cell-free assays. Nocodazole binds to beta-tubulin and disrupts microtubule assembly/disassembly dynamics.
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.
T3068 AT9283 AT9283 is an effective multi-targeted inhibitor of JAK2(IC50=1.2 nM) and JAK3(IC50=1.1 nM), Aurora A, Aurora B and Abl(T315I).
T3071 GZD824 GZD824 is an orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT, IC50: 0.34 nM) and Bcr-Abl(T315I, IC50: 0.68 nM).
T3196 GNF-7 GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.
T3641 BAW2881 BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation.
T3697 3,6'-Disinapoyl sucrose 3,6'-Disinapoyl sucrose shows the neuroprotective effect and antidepressive activity in rats.
T3706 BDA-366 BDA-366 specifically targets the BH4 domain of Bcl2 BDA-366 and suppresses human myeloma growth. BDA-366 induces robust apoptosis in MM cell lines and primary MM cells by inducing BCL2 conformational change. Delivery of BDA-366 substantially suppressed the growth of human MM xenografts in NOD-scid/I
T3864 Erianin Erianin is a nature product extracted from Dendrobium chrysotoxum, has notable antitumour activity , can cause extensive tumour necrosis, growth delay. Erianin has antiangiogenic action by inhibiting endothelial metabolism in a JNK/SAPK-dependent manner and inducing endothelial cytoskeletal disorgan
T3867 Alpinetin Alpinetin has antibacterial activity. Alpinetin has anti-inflammatory activity. Alpinetin can enhance the sensitivity of HepG2 hepatoma cells to the chemotherapeutic agent CDDP. Alpinetin has strong anti-hepatoma and pancreatic cancer cells effects, by inhibiting proliferation ,regulating of the Bcl
T3940 CID5721353 <p>ID5721353 is a B-Cell Lymphoma 6 Inhibitor (BCL6 inhibitor).</p>
T4088 Thymoquinon Thymoquinon is a compound be found in herbs and spices with anti-inflammatory and anti-oxidant effects.
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).
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).
T6128 PHA-665752 PHA-665752 is an effective, specific and ATP-competitive c-Met inhibitor (IC50: 9 nM), >50-fold selectivity for c-Met than STKs or RTKs.
T6185 Gambogic Acid Gambogic Acid ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.
T6196 PP1 PP1, a specific and effective Src inhibitor, is with IC50 for Lck/Fyn is 5 nM/ 6 nM, respectively.
T6230 Imatinib (STI571) Imatinib is a tyrosine kinase inhibitor and ANTINEOPLASTIC AGENT that inhibits the BCR-ABL kinase created by chromosome rearrangements in CHRONIC MYELOID LEUKEMIA and ACUTE LYMPHOBLASTIC LEUKEMIA, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors.
T6275 Obatoclax Mesylate Obatoclax (GX15-070) is an Bcl-2 antagonist (Ki: 0.22 μM), can assist in overcoming MCL-1 mediated resistance to apoptosis.
T6281 TW-37 TW-37 is an nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 (Ki: 0.29/1.11/0.26 μM).
T6300 WP1130 Degrasyn (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr/Abl, which is a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).
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.
T6314 AT101 AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM.
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.
T6396 AT101 acetate AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID. Phase 2.
T6650 Sabutoclax Sabutoclax(BI-97C1) is a pan-Bcl-2 inhibitor, including Bcl-xL, Bcl-2, Mcl-1 and Bfl-1 with IC50 of 0.31 μM, 0.32 μM, 0.20 μM and 0.62 μM, respectively.
T6748 A-1155463 A-1155463, a highly potent and selective BCL-XL inhibitor, shows picomolar binding affinity to BCL-XL, and >1000-fold weaker binding to BCL-2 and related proteins BCL-W(Ki=19 nM) and MCL-1(Ki>440 nM).
T6749 A-1331852 A-1331852 is a potent and selectiveBCL-XL inhibitor and may be useful in the treatment of cancer, immune and autoimmune diseases.
T4320 Flumatinib Flumatinib is an orally bioavailable tyrosine kinase inhibitor flumatinib, with potential antineoplastic activity.
  • 关注公众号
    - 超值特惠
    - 客户福利
    - 业界动态
    - 实用攻略
陶素的所有产品和服务仅用于科研,我们不为任何其他用途提供产品和服务