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a line wedding dress
ys123
38 posts Dec 23, 2011
4:14 AM
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xuefei
Guest Jan 12, 2012
10:42 PM
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Anonymous
Guest Feb 02, 2012
1:02 PM
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MDV3100 is an androgen-receptor (AR) antagonist with IC50 of 36 nM. MDV3100 has greater affinity to AR than bicalutamide does in a competition assay with 16?-[18F]fluoro-5?-DHT (18-FDHT). MDV3100 shows no agonism in LNCaP/AR (AR-overexpressing) prostate cells. MDV3100 antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. MDV3100 could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). AC220 (Quizartinib) is a uniquely potent and selective FLT3 inhibitor with IC50 of 0.56 ± 0.3 nM and >10 mM for MC4-11 and A375, respectively. AC220 exhibits low nanomolar potency in biochemical and cellular assays and exceptional kinase selectivity, and in animal models is efficacious at doses as low as 1 mg/kg given orally once daily. The data reveal that the combination of excellent potency, selectivity, and pharmacokinetic properties is unique to AC220, which therefore is the first candidate with a profile that matches the characteristics desirable for a clinical FLT3 inhibitor.In contrast, Linifanib (ABT-869) had only weak activity (IC50 > 1 ?M) against cells whose proliferation is not driven by a VEGF or PDGF tyrosine kinase, such as HT-29 and MDA-435 carcinoma cells. Antiproliferative effects in these cellular assays is observed at >1,000-fold higher Linifanib (ABT-869) concentrations than in the VEGF-stimulated HUAEC assay. ABT-869 does potently inhibit the proliferation of MV4-11 leukemia cells which are known to express a constitutively active form of FLT3, with an IC50 of 4 nM.KU-55933 is a potent and specific ATM inhibitor with an IC50 and a Ki of 13 and 2.2 nM, respectively. KU-55933 reveals specificity with respect to prevention the phosphatidylinositol 3-kinase-like kinases. Exposure of cells to KU-55933 led to a markedly sensitization to the cytotoxic effects of ionizing radiation and to the DNA double-strand break-inducing chemotherapeutic agents, etoposide, doxorubicin, and camptothecin. AZD6244 (Selumetinib) is highly potent to inhibit MEK1 with IC50 of 14nmol. AZD6244 is a not competitive with ATP and inactivates the ERK1/2 phosphorylation with IC50 concentrations below 40 nmol. AZD6244 also inhibits the growth of primary HCC cells through inhibition of ERK1/2 and p90RSK phosphorylation, accompanied with elevation of the cleavage of caspase-3 and caspase-7, and cleaved poly(ADP)ribose polymerase.
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Anonymous
Guest Feb 04, 2012
7:54 AM
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Anonymous
Guest Feb 04, 2012
7:57 AM
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Anonymous
Guest Feb 04, 2012
7:58 AM
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