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[CAS NO. 186692-46-6] (R)-Roscovitine
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-30237 |
| Brand: | MCE |
| CAS: | 186692-46-6 |
Overview
| MDL | MFCD02266401 |
|---|---|
| Molecular Weight | 354.45 |
| Molecular Formula | C19H26N6O |
| SMILES | OC[C@H](NC1=NC(NCC2=CC=CC=C2)=C3C(N(C=N3)C(C)C)=N1)CC |
18 Publications Citing Use of MCE
- [1]Nature. 2020 Sep;585(7824):293-297.
- [2]Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
- [3]Cell Death Differ. 2021 Jan;28(1):337-348.
- [4]Redox Biol. 22 July 2022, 102418.
- [5]Cell Syst. 2018 Apr 25;6(4):424-443.e7.
- [6]Cell Rep. 2021 Jul 20;36(3):109394.
- [7]J Med Chem. 2021 Mar 11;64(5):2725-2738.
- [8]Br J Cancer. 2023 Jan 30.
- [9]Neoplasia. 2018 Mar 28;20(5):478-488.
- [10]Mol Cancer Res. 2020 Jan;18(1):91-104.
- [11]Oncol Rep. 2020 Jan;43(1):306-317.
- [12]Biochimie. 2020 Jan;168:277-284.
- [13]Eur J Pharmacol. 1 July 2022, 175118.
- [14]Virology. 2021 May 22.
- [15]Neuroreport. 2018 Mar 7;29(4):241-246.
- [16]Chin J Org Chem. 2017, 37 (6): 1479-1486.
- [17]Chin J Org Chem. 2016, 36(5): 1044-1050.
- [18]Harvard Medical School LINCS LIBRARY
Summary
IC50 & Target
|
cdc2/cyclin B 0.65 μM (IC 50 ) |
cdk2/cyclin A 0.7 μM (IC 50 ) |
Cdk2/cyclin E2 0.7 μM (IC 50 ) |
CDK5/p35 0.16 μM (IC 50 ) |
GST-erk1 30 μM (IC 50 ) |
erk1 34 μM (IC 50 ) |
||||
|
erk2 14 μM (IC 50 ) |
IR tyrosine kinase 70 μM (IC 50 ) |
||||||||
In Vitro
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 (IC 50 values of 0.65, 0.7, and 0.2 μM, respectively). Cdk4k and Cdk6 are very poorly inhibited by Seliciclib (Roscovitine) (IC 50 >100 μM). Extracellular regulated kinases erk1 and erk2 are inhibited with an IC 50 of 34 μM and 14 μM, respectively. Seliciclib (Roscovitine) inhibits the proliferation of mammalian cell lines with an average IC 50 of 16 μM [1] . 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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 [2] . 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 [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02649751 | University Hospital, Brest|ManRos Therapeutics|Cyclacel Pharmaceuticals, Inc. |
Cystic Fibrosis
|
February 22, 2016 | Phase 2 |
| NCT02160730 | Shlomo Melmed, MD|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Cedars-Sinai Medical Center |
Cushings Disease
|
May 2014 | Phase 2 |
| NCT03774446 | Cedars-Sinai Medical Center |
Cushing Disease
|
November 2, 2018 | Phase 2 |
| NCT01333423 | M.D. Anderson Cancer Center|National Institutes of Health (NIH) |
Breast Cancer
|
September 2012 | Phase 1 |
| NCT00999401 | Cyclacel Pharmaceuticals, Inc. |
Advanced Solid Tumors
|
April 2009 | Phase 1 |
| NCT00372073 | Cyclacel Pharmaceuticals, Inc. |
Non-small Cell Lung Cancer
|
August 9, 2006 | Phase 2 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 282.13 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.8213 mL | 14.1064 mL | 28.2127 mL |
| 5 mM | 0.5643 mL | 2.8213 mL | 5.6425 mL |
| 10 mM | 0.2821 mL | 1.4106 mL | 2.8213 mL |
-
1.
Add each solvent one by one: 10% DMSO >> 90% saline
Solubility: 5 mg/mL (14.11 mM); Suspended solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution
-
5.
-
6.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution
References
- [1] Meijer L, et al. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem. 1997 Jan 15;243(1-2):527-36.
- [2] Bai X, et al. CDK5 promotes renal tubulointerstitial fibrosis in diabetic nephropathy via erk1/2/pparγ pathway. Oncotarget. 2016 Apr 27.
- [3] Gary C, et al. Selective antitumor activity of roscovitine in head and neck cancer. Oncotarget. 2016 May 23.
Synonyms
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