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Roscovitine (Seliciclib)

Cat. No. M1974
Roscovitine (Seliciclib) Structure
Synonym:

Seliciclib, CYC202

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 45  USD45 In stock
10mg USD 77  USD77 In stock
50mg USD 170  USD170 In stock
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Quality Control & Documentation
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.

Product Citations
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.
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.
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.
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.
Chemical Information
Molecular Weight 354.45
Formula C19H26N6O
CAS Number 186692-46-6
Solubility (25°C) DMSO 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Rossi AG, et al. Nat Med. Cyclin-dependent kinase inhibitors enhance the resolution of inflammation by promoting inflammatory cell apoptosis.

[2] MacCallum DE, et al. Cancer Res. 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.

[3] Raje N, et al. Blood. Seliciclib (CYC202 or R-roscovitine), a small-molecule cyclin-dependent kinase inhibitor, mediates activity via down-regulation of Mcl-1 in multiple myeloma.

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Keywords: Roscovitine (Seliciclib), Seliciclib, CYC202 supplier, CDK, inhibitors, activators


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