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Roscovitine

Cat. No. M1974
Roscovitine Structure
Synonym:

Seliciclib, CYC202

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 200 In stock
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Quality Control
Biological Activity

Roscovitine (Seliciclib or CYC202) is a cyclin-dependent kinase (CDK) inhibitor that preferentially inhibits multiple enzyme targets including CDK2, CDK7 and CDK9, which alter the growth phase or state within the cell cycle of treated cells. Cyclin-dependent kinases (cdk) play an essential role in the intracellular control of the cell division cycle (cdc). Seliciclib has been shown to inhibit RNA polymerase II-dependent transcription and down-regulation of the protein MCL1. Roscovitine inhibits in vitro M-phase-promoting factor activity and in vitro DNA synthesis in Xenopus egg extracts. It blocks progesterone-induced oocyte maturation of Xenopus oocytes and in vivo phosphorylation of the elongation factor eEF-1. Roscovitine inhibits the proliferation of mammalian cell lines with an average IC50 of 16 microM. At 20 microM, Roscovitine induced apoptosis in 21 of 28 B-CLL samples and was equally effective in zap-70-positive or -negative samples. Caspase-3 was cleaved in B-CLL cells exposed to Roscovitine and the pancaspase inhibitor z.VAD.fmk-blocked Roscovitine-induced apoptosis. Roscovitine induced a block in G1 earlier than that induced by aphidicolin. S-phase synchronized cells treated with roscovitine were arrested at a 4C DNA content at the G2/ M transition. Finally, cells in metaphase were insensitive to roscovitine. The purified CDK/cyclin kinase activities of late G1 and early M arrested cells were inhibited in vitro by roscovitine.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 354.45
Formula C19H26N6O
CAS Number 186692-46-6
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source Discov Med (2017). Figure 5. Roscovitine (Abmole Bioscience, Houston, TX)
Method Western blot
Cell Lines Sprague-Dawley rats
Concentrations 5 mg/kg
Incubation Time 24 h
Results PTZ-kindled rats had increased level of Cdk5 in white matters, memantine, ifenprodil, lithium chloride (LiCl), and roscovitine decreased Cdk5 in PTZ-kindled rats.
Rating
Source Discov Med (2017). Figure 4. Roscovitine (Abmole Bioscience, Houston, TX)
Method Immunohistochemistry
Cell Lines Sprague-Dawley rats
Concentrations 5 mg/kg
Incubation Time 24 h
Results Representative immunohistochemical microphotographs showed increased accumulation of APP in corpus callosum in PTZ-kindled rats. Memantine, ifenprodil, lithium chloride (LiCl), and roscovitine alleviated the accumulation.
Rating
Source Discov Med (2017). Figure 3. Roscovitine (Abmole Bioscience, Houston, TX)
Method Immunohistochemistry
Cell Lines Sprague-Dawley rats
Concentrations 5 mg/kg
Incubation Time 24 h
Results Memantine, ifenprodil, lithium chloride (LiCl), and roscovitine alleviated such reduction.
Rating
Source Discov Med (2017). Figure 2. Roscovitine (Abmole Bioscience, Houston, TX)
Method Western blot
Cell Lines Sprague-Dawley rats
Concentrations 5 mg/kg
Incubation Time 24 h
Results Roscovitine decreased relative tau phosphorylation level and the level of p-tau S396 and p-tau T231 without increase of total tau.
Rating
Product Citations
References

Cyclin-dependent kinase inhibitors enhance the resolution of inflammation by promoting inflammatory cell apoptosis.
Rossi AG, et al. Nat Med. 2006 Sep;12(9):1056-64. PMID: 16951685.

Seliciclib (CYC202, R-Roscovitine) induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1.
MacCallum DE, et al. Cancer Res. 2005 Jun 15;65(12):5399-407. PMID: 15958589.

Seliciclib (CYC202 or R-roscovitine), a small-molecule cyclin-dependent kinase inhibitor, mediates activity via down-regulation of Mcl-1 in multiple myeloma.
Raje N, et al. Blood. 2005 Aug 1;106(3):1042-7. PMID: 15827128.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Roscovitine, Seliciclib, CYC202 supplier, CDK, inhibitors

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