[CAS NO. 186692-46-6] (R)-Roscovitine

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PRODUCTS SPECIFICATIONS [186692-46-6]

Catalog

HY-30237

Brand

MCE

CAS

186692-46-6

DESCRIPTION [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

For research use only. We do not sell to patients.

18 Publications Citing Use of MCE

Summary

Seliciclib (Roscovitine) is an orally bioavailable and selective CDKs inhibitor with IC ₅₀ s of 0.2 μM, 0.65 μM, and 0.7 μM for CDK5 , Cdc2 , and CDK2 , respectively.

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

In Vitro:

DMSO : ≥ 100 mg/mL ( 282.13 mM )

* "≥" means soluble, but saturation unknown.

Preparing
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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% saline

Solubility: 5 mg/mL (14.11 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution
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.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (7.05 mM); Clear solution
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

* All of the co-solvents are available by MCE.

References

Synonyms

1-Butanol, 2-[[9-(1-methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-, (2R)-

1-Butanol, 2-[[9-(1-methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-, (R)-

(2R)-2-[[9-(1-Methylethyl)-6-[(phenylmethyl)amino]-9H-purin-2-yl]amino]-1-butanol

Roscovitine

CYC 202

R-Roscovitine

Seliciclib

2-(R)-(1-Ethyl-2-hydroxyethylamino)-6-benzylamino-9-isopropylpurine

Roscovitin

(R)-Roscovitine

(2R)-2-[[6-(Benzylamino)-9-propan-2-ylpurin-2-yl]amino]butan-1-ol