>>

>>

抑制剂/激活剂

>>

凋亡与自噬

>>

Seliciclib Roscovitine; CYC202; R-roscovitine

Seliciclib (Roscovitine) 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。

货号：
TK0233
规格：

5mg

10mg

50mg
价格：
￥0.00

产品参数

CAS No.	186692-46-6
生物活性	Seliciclib (Roscovitine) is an orally bioavailable and selective CDKs inhibitor with IC50s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5, Cdc2, and CDK2, respectively.
分子式	C19H26N6O
分子量	354.45
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	Powder -20°C 3 years
溶解性数据	DMSO : ≥ 100 mg/mL (282.13 mM)
体内研究	Compare with normal controls, Seliciclib (Roscovitine) downregulates phosphorylated ERK1/2 and PPARγ with concomitant increase in E-cadherin, but decrease in Vimentin and Collagen IV. Correspondingly, Seliciclib decreases renal tubulointerstitial fibrosis of diabetic rats. Seliciclib (Roscovitine) is effective in decreasing tubulointerstitial fibrosis via the ERK1/2/PPARγ pathway in diabetic rats. Seliciclib (Roscovitine) (16.5 mg/kg) significantly reduces the rate of tumor growth and increases survival of treated mice. Strikingly, Seliciclib (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 Seliciclib and control mice, and behavioral differences between the two groups are also negligible. These results suggest that Seliciclib can be used effectively as a selective tumor growth inhibitor in HPV+ head and neck cancer.
体外研究	Seliciclib (Roscovitine) 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 Seliciclib (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 Seliciclib (Roscovitine) (IC50>100 μM). Extracellular regulated kinases erk1 and erk2 are inhibited with an IC50 of 34 μM and 14 μM, respectively. Seliciclib (Roscovitine) inhibits the proliferation of mammalian cell lines with an average IC50 of 16 μM. Seliciclib decreases the level of CDK5 and p35 with upregulation of E-cadherin, but downregulation of Vimentin and Collagen IV. Moreover, Seliciclib (Roscovitine) inhibits the ability of high glucose cultured NRK52E cells to migrate and invade.
文献	•Nature. 2020 Sep;585(7824):293-297. •Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •Cell Death Differ. 2021 Jan;28(1):337-348. •Cell Rep. 2021 Jul 20;36(3):109394. •Cell Syst. 2018 Apr 25;6(4):424-443.e7. •J Med Chem. 2021 Feb 23. •Mol Cancer Res. 2020 Jan;18(1):91-104. •Neoplasia. 2018 Mar 28;20(5):478-488. •Oncol Rep. 2020 Jan;43(1):306-317. •Biochimie. 2020 Jan;168:277-284. •Virology. 2021 May 22. •Neuroreport. 2018 Mar 7;29(4):241-246. •Chin J Org Chem. 2017, 37 (6): 1479-1486. •Chin J Org Chem. 2016, 36(5): 1044-1050. •Harvard Medical School LINCS LIBRARY
纯度及产品资料	98%

推荐产品