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(R)-Roscovitine

CAS No. : 186692-46-6

MCE 站：(R)-Roscovitine

产品活性：(R)-Roscovitine (Seliciclib) 是一种有效的，具有口服活性的，选择性的 CDKs 抑制剂，抑制 CDK5，Cdc2 和 CDK2 的 IC₅₀ 分别为0.2 μM，0.65 μM，0.7 μM。

研究领域：Cell Cycle/DNA Damage

作用靶点：CDK

In Vitro: (R)-Roscovitine (Seliciclib) displays high efficiency ａnd high selectivity towards some cyclin-dependent kinases. The kinase specificity of Seliciclib is investigated with 25 highly purified kinases (including protein kinase A, G ａnd C isoforms, myosin light-chain kinase, casein kinase 2, IR tyrosine kinase, c-src, v-abl). Most kinases are not significantly inhibited by (R)-Roscovitine. Cdc2, Cdk2, ａnd Cdk5 only are substantially inhibited (IC₅₀ values of 0.65, 0.7, ａnd 0.2 μM, respectively). Cdk4k ａnd Cdk6 are very poorly inhibited by (R)-Roscovitine (IC₅₀>100 μM). Extracellular regulated kinases erk1 ａnd erk2 are inhibited with an IC₅₀ of 34 μM ａnd 14 μM, respectively. (R)-Roscovitine inhibits the proliferation of mammalian cell lines with an average IC₅₀ of 16 μM. (R)-Roscovitine (Seliciclib) decreases the level of CDK5 ａnd p35 with upregulation of E-cadherin, but downregulation of Vimentin ａnd Collagen IV. Moreover, (R)-Roscovitine inhibits the ability of high glucose cultured NRK52E cells to migrate ａnd invade.

In Vivo: Compare with normal controls, (R)-Roscovitine (Seliciclib) downregulates phosphorylated ERK1/2 ａnd PPARγ with concomitant increase in E-cadherin, but decrease in Vimentin ａnd Collagen IV. Correspondingly, (R)-Roscovitine decreases renal tubulointerstitial fibrosis of diabetic rats. (R)-Roscovitine is effective in decreasing tubulointerstitial fibrosis via the ERK1/2/PPARγ pathway in diabetic rats. (R)-Roscovitine (Seliciclib) (16.5 mg/kg) significantly reduces the rate of tumor growth ａnd increases survival of treated mice. Strikingly, (R)-Roscovitine treatment leads to complete tumor disappearance in one mouse (25%); moreover, no tumor regrowth in this mouse is found 5 months after completion of the treatment. Mouse weights do not differ significantly between mice treated with (R)-Roscovitine ａnd control mice, ａnd behavioral differences between the two groups are also negligible. These results suggest that (R)-Roscovitine can be used effectively as a selective tumor growth inhibitor in HPV+ head ａnd neck cancer.

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