Purvalanol B (Synonyms: NG 95; NG95; NG-95) |
| Catalog No.GC16268 |
CDK1/CDK2/CDK4 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 212844-54-7
Sample solution is provided at 25 µL, 10mM.
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Purvalanol B is a selective inhibitor of CDK1, CDK2 and CDK4.
CDKs (cyclin-dependent kinases) family has the ability to regulate cell cycle.
Purvalanol B is reported as one of the most potent and selective CDK inhibitors. When tested with Chinese hamster lung fibroblast CCL39 cell line, treatment with Purvalanol B inhibited cells proliferate via targeting CKD1 which induced a G2/M block with a GI50 of 2.5 μM. In asynchronous cells, exposed to Purvalanol B led to an accumulation of cells in G2/M phase [1].
In a mouse model with NCI-H2228 subcutaneous xenograft, oral administration of ASP3026 caused significant reduction of phosphorylated ALK and tumor growth. 30 mg/kg/d ASP3026 for 2 weeks induced tumor regression by 78%. In mice injected with Karpas 299 cells, ASP3026 treatment caused remarkable lymphoma regression [2, 3].
Purvalanol B also interacts with p42/p44 MAPK proteins when tested with several mammalian cell lines including MCF-7 cell line [1].
References:
1.Kuromitsu S, Mori M, Shimada I, et al. Anti-tumor activity of ASP3026, a novel and selective ALK inhibitor of anaplastic lymphoma kinase (ALK). Annual Meeting of the American Association for Cancer Research (AACR), Orlando, FL. 2011.
2.Mori M, Ueno Y, Konagai S, et al. The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice. Molecular cancer therapeutics, 2014, 13(2): 329-340.
3.George S K, Vishwamitra D, Manshouri R, et al. The ALK inhibitor ASP3026 eradicates NPM-ALK+ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget, 2014, 5(14): 5750-5763.
| Cell experiment [1]: | |
|
Cell lines |
Chinese hamster lung fibroblast CCL39 cell line, Asynchronous cells |
|
Preparation method |
The solubility of this compound in DMSO is >21.7mg/mL. 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. |
|
Reacting condition |
2.5 μM |
|
Applications |
In Chinese hamster lung fibroblast CCL39 cell line, treatment with Purvalanol B inhibited cells proliferation via targeting CKD1 which induced a G2/M block with a GI50 of 2.5 μM. In asynchronous cells, Purvalanol B led to an accumulation of cells in G2/M phase. |
| Animal experiment [2, 3]: | |
|
Animal models |
Mouse model with NCI-H2228 subcutaneous xenograft and Karpas 299 cells |
|
Dosage form |
Oral administration, 30 mg/kg/d, 2 weeks |
|
Application |
In a mouse model with NCI-H2228 subcutaneous xenograft, oral administration of ASP3026 significantly reduced phosphorylated ALK and tumor growth. ASP3026 (30 mg/kg/d, 2 weeks) induced tumor regression by 78%. In mice injected with Karpas 299 cells, ASP3026 treatment caused remarkable lymphoma regression。 |
|
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]. Kuromitsu S, Mori M, Shimada I, et al. Anti-tumor activity of ASP3026,–A novel and selective ALK inhibitor[J]. 2011. [2]. Mori M, Ueno Y, Konagai S, et al. The Selective Anaplastic Lymphoma Receptor Tyrosine Kinase Inhibitor ASP3026 Induces Tumor Regression and Prolongs Survival in Non–Small Cell Lung Cancer Model Mice. Molecular cancer therapeutics, 2014, 13(2): 329-340. [3].George S K, Vishwamitra D, Manshouri R, et al. The ALK inhibitor ASP3026 eradicates NPM-ALK+ T-cell anaplastic large-cell lymphoma in vitro and in a systemic xenograft lymphoma model. Oncotarget, 2014, 5(14): 5750-5763. |
|
| Cas No. | 212844-54-7 | SDF | |
| Synonyms | NG 95; NG95; NG-95 | ||
| Chemical Name | 2-chloro-4-[[2-[[(2R)-1-hydroxy-3-methylbutan-2-yl]amino]-9-propan-2-ylpurin-6-yl]amino]benzoic acid | ||
| Canonical SMILES | CC(C)C(CO)NC1=NC2=C(C(=N1)NC3=CC(=C(C=C3)C(=O)O)Cl)N=CN2C(C)C | ||
| Formula | C20H25ClN6O3 | M.Wt | 432.9 |
| Solubility | ≥ 21.65mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.31 mL | 11.55 mL | 23.1 mL |
| 5 mM | 0.462 mL | 2.31 mL | 4.62 mL |
| 10 mM | 0.231 mL | 1.155 mL | 2.31 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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