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Dinaciclib(SCH727965) Sale

(Synonyms: (2S)-1-[3-乙基-7-[[(1-氧代-3-吡啶基)甲基]氨基]吡唑并[1,5-A]嘧啶-5-基]-2-哌啶乙醇,SCH 727965) 目录号 : GC17648

A CDK inhibitor

Dinaciclib(SCH727965) Chemical Structure

Cas No.:779353-01-4

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥704.00
现货
5mg
¥935.00
现货
25mg
¥2,541.00
现货
50mg
¥3,444.00
现货

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

Cyclin/CDK kinase assay

Recombinant cyclin/CDK holoenzymes were purified from Sf9 cells engineered to produce baculoviruses that express a specific cyclin or CDK. Cyclin/CDK complexes were typically diluted to a final concentration of 50 μg/mL in a kinase reaction buffer containing 50 mmol/L Tris-HCl (pH 8.0), 10 mmol/L MgCl2, 1 mmol/L DTT, and 0.1 mmol/L sodium orthovanadate. For each kinase reaction, 1 μg of enzyme and 20 μL of a 2-μmol/L substrate solution (a biotinylated peptide derived from histone H1; Amersham) were mixed and combined with 10 μL of diluted SCH 727965. The reaction was started by the addition of 50 μL of 2 μmol/L ATP and 0.1 μCi of 33P-ATP. Kinase reactions were incubated for 1 hour at room temperature and were stopped by the addition of 0.1% Triton X-100, 1 mmol/L ATP, 5 mmol/L EDTA, and 5 mg/mL streptavidin-coated SPA beads. SPA beads were captured using a 96-well GF/B filter plate and a Filtermate universal harvester. Beads were washed twice with 2 mol/L NaCl and twice with 2 mol/L NaCl containing 1% phosphoric acid. The signal was then assayed using a Top-Count 96-well liquid scintillation counter. Dose-response curves were generated from duplicate, eight-point serial dilutions of inhibitory compounds. IC50 values were derived by nonlinear regression analysis.

Cell experiment [1]:

Cell lines

A2780 cells

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

2 h

Applications

SCH 727965 significantly abrogates phosphorylation of Rb on Ser 807/811 at concentrations >6.25 nmol/L and also leads to the generation of the p85 PARP cleavage product. 100 nmol/L SCH727965 treatment for 2 hours is effective in inducing suppression of Rb phosphorylation and caspase activation which can be detected up to 6 hours later.

Animal experiment [1]:

Animal models

A2780 ovarian cancer mouse xenograft model

Dosage form

i.p. administration at 8, 16, 32, and 48 mg/kg daily

Applications

SCH 727965 i.p. administration at 8, 16, 32, and 48 mg/kg daily for 10 days shows tumor inhibitionby 70%, 70%, 89%, and 96%, respectively. SCH 727965 is also well tolerated, and the maximum body weight loss in the highest dosage group is 5%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Parry D, Guzi T, Shanahan F et al. Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53.

产品描述

Dinaciclib is a potent cyclin-dependent kinase (CDK) inhibitor with IC50s for CDK2, CDK5, CDK1 and CDK9 at 1 nM, 1 nM, 3 nM, and 4 nM, respectively. [1] It is in phase I or II clinical trials for various cancers.

Dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. [2] Inhibition of CDK 1 suppresses Rb phosphorylation, leading to cell cycle arrest and apoptosis. [3]

Dinaciclib is active against a broad spectrum of human tumor cell lines in vitro and in vivo. It has great potential to improve cancer chemotherapy.

References:
[1]Parry D., et al. (2010). Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor. Mol Cancer Ther (9): 2344- 2353.
[2]Martin, M. P., et al. (2013). Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. ACS Chemical Biology 8 (11): 2360–5.
[3]Payton M., et al. (2006). Discovery and Evaluation of Dual CDK1 and CDK2 Inhibitors. Cancer Res 66: 4299-4308.

Chemical Properties

Cas No. 779353-01-4 SDF
别名 (2S)-1-[3-乙基-7-[[(1-氧代-3-吡啶基)甲基]氨基]吡唑并[1,5-A]嘧啶-5-基]-2-哌啶乙醇,SCH 727965
化学名 2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol
Canonical SMILES CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCCC4CCO
分子式 C21H28N6O2 分子量 396.49
溶解度 ≥ 17.15mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.5221 mL 12.6107 mL 25.2213 mL
5 mM 0.5044 mL 2.5221 mL 5.0443 mL
10 mM 0.2522 mL 1.2611 mL 2.5221 mL
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