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eliwu's blog / Uncategorized / JNJ-38877605 is a c-MET inhibitor with an IC50 of 4 nM
JNJ-38877605 is a c-MET inhibitor with an IC50 of 4 nM
27 June, 201127 June, 2011 3 comments Uncategorized Uncategorized

NVP-BEP800 is a novel, fully synthetic, oral Hsp90 inhibitor with an IC50 of 0.058

± 0.006 μM.Want know more about Hsp90 inhibitors

NVP-BEP800

JNJ-38877605 is a c-MET inhibitor with an IC50 of 4 nM.Know more c-met inhibitors

JNJ-38877605

GDC-0879 is an B-Raf inhibitor( EC50 = 0.75 μM).

GDC-0879

ABT-737 is a pan-Bcl-2 inhibitor and ABT-737 ingle-agent LC90 values ranged from 100 nM for COG-LL-319.learn more bcl-2 inhibitors.

apoptosis inhibitor is the process of programmed cell death.CDK inhibitor with an IC50 of 0.011 μM for Cdk4 and IC50 of 0.016 μM for Cdk6.

Assessment of the effect of various oral doses of erlotinib on tumor growth in the HN5 head and neck tumor xenograft model indicated a marked improvement in antitumor effect between doses of 1.6 and 12.5 mg/kg.

erlotinib

IC50 (μM):PARP-1= 0.005,PARP-2= 0.001 , PF50=25.8.AZD2281(Olaparib) at 400 mg twice daily is well tolerated and highly active.

Sunitinib Malate (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 μM for Flk-1 and PDGFR, respectively.

 

 

Gefitinib inhibits AKT phosphorylations, with IC50 values of 220 and 263 nM, in the low-EGFR- and –EGFRvIII-expressing cell lines, respectively.

such as: apoptosis inhibitors, cdk inhibitors,

MDV3100Biological Activity of Nilotinib(Tasigna):
Chronic myelogenous leukaemia (CML) and Philadelphia chromosome positive (Ph+) acute lymphoblastic leukaemia (ALL) are caused by the BCR-ABL oncogene.read more...

Lenalidomide is a derivative of thalidomide with antiangiogenic and antineoplastic properties(cell IC50= 10 μM). learn more...

Lenalidomide

MDV3100 is an androgen-receptor antagonist that blocks androgens from binding to the androgen receptor and prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex. more info...

MDV3100

Temsirolimus has shown promising preclinical and early clinical antitumor activity and is currently in phase III clinical development for the treatment of different solid tumors, including breast cancer.

Temsirolimus

 

Colony forming capability of MES-SA cells treated with 3 μM vorinostat for 24 and 48 hours was significantly diminished and blocked after 72 hours.Vorinostat

Neratinib is an orally available, irreversible tyrosine kinase inhibitor with IC50 of 59 nM and 92 nM for HER2 and EGFR, respectively.

The dipeptide boronic acid inhibitor bortezomib effectively inhibits proteasome activity (Ki-0.6 nM) but has little affinity for other proteases (e.g., for chymotrypsin, Ki=320 nM, and for thrombin, Ki=13,000 nM).know more...

Dasatinib is a potent inhibitor of imatinib-resistant KIT activation loop mutants and induces apoptosis in mast cell and leukemic cell lines expressing these mutations.

Pazopanib showed good potency against all the human VEGFR receptors with an IC50 of 10, 30, and 47 nM for VEGFR-1, -2, and -3, respectively.

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