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PIK-90

CAS No. : 677338-12-4

MCE 站：PIK-90

产品活性：PIK-90 是一种 PI3K 和 DNA-PK 抑制剂，抑制 p110α, p110γ，和 DNA-PK，IC₅₀ 分别为 11, 18 和 13 nM。

研究领域：PI3K/Akt/mTOR  |  Cell Cycle/DNA Damage

作用靶点：PI3K  |  DNA-PK

In Vitro: PIK-90 also inhibits p110β, p110δ, PI3KC2α, PI3KC2β, hsVPS34, PI4KIIIα, PI4KIIIβ, ATR, ATM and mTORC1 with IC₅₀s of 350 nM, 58 nM, 47 nM, 64 nM, 830 nM, 830 nM, 3.1 μM, 15 μM, 610 nM and 1.05 μM, respectively. To determine the effects of PIK-90 on chronic lymphocytic leukemia (CLL) cell viability, CLL cells from different patients are incubated with various concentrations of PIK-90 (1 μM and 10 μM) for 24, 48, and 72 hours. PIK-90 reveals the strong apoptosis-inducing effects at both concentrations and at all different time points. Using a concentration of 10 μM, PIK-90 reduces the viability of CLL cells to 51.1% plus or minus 6.6% at 24 hours, whereas 1 μM PIK-90 reduces the viability to 77.8% plus or minus 6.4%.

In Vivo: To test the efficacy of Roscovitine and PIK-90 in vivo, GBM43 cells are implanted s.c. into nude mice. Mice with established tumors are randomized into four treatment groups: vehicle (PBS:H₂O), Roscovitine, PIK-90, or PIK-90 plus Roscovitine. After 12 d of treatment, both Roscovitine and PIK-90 show clear single-agent efficacy, with tumor size in mice treated with Roscovitine and PIK-90 in combination significantly smaller than either vehicle or monotherapy-treated controls. Roscovitine is less effective than PIK-90 in blocking proliferation (levels of Ki-67), whereas combination therapy shows essentially additive antiproliferative effects.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  3-Methyladenine  |  LY294002  |  Wortmannin  |  Quercetin  |  740 Y-P  |  PI-103  |  Isorhamnetin  |  Recilisib  |  Autophinib  |  AZD 6482  |  PI3K-IN-1  |  TG100-115  |  α-Linolenic acid  |  TGX-221  |  1-Deoxynojirimycin  |  YS-49  |  AS-605240  |  PKI-402  |  Disitertide  |  LTURM34  |  Erucic acid  |  CNX-1351  |  GSK1059615  |  Sonolisib  |  1,3-Dicaffeoylquinic acid  |  GNE-317  |  Esculetin  |  HS-173

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