GZD824 (Synonyms: GZD824 dimesylate; HQP1351 dimesylate) |
| カタログ番号GC10915 |
オルベレンマチニブ (GZD824) ジメシラートは、経口で有効な汎 Bcr-Abl 阻害剤です。 GZD824 は、広範囲の Bcr-Abl 変異体を強力に阻害します。 ＧＺＤ８２４は、天然のＢｃｒ－ＡｂｌおよびＢｃｒ－ＡｂｌＴ３１５Ｉを、それぞれ０．３４ｎＭおよび０．６８ｎＭのＩＣ５０で強力に阻害する。 GZD824 には抗腫瘍活性があります。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1421783-64-3
Sample solution is provided at 25 µL, 10mM.
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GZD824 is an orally bioavailable inhibitor of Bcr-Abl with IC50 values of 0.34 and 0.68 nM for Bcr-AblWT and Bcr-AblT315I, respectively [1].
Bcr-Abl is a fused protein that interacts with the interleukin-3 receptorβ(c) subunit and has tyrosine kinase activity. Abl activates cell cycle-related proteins and enzymes and increases cell division. Bcr-Abl inhibits DNA repair and causes genomic instability.
GZD824 is an orally bioavailable Bcr-Abl inhibitor. GZD824 exhibited high affinity with Kd values of 0.32 and 0.71 nM for Bcr-AblWT and Bcr-AblT315I, respectively. GZD824 inhibited Bcr-Abl with IC50 values of 0.34, 0.68, 0.27, 0.71, 0.15, 0.35, 0.29 and 0.35 nM for Bcr-AblWT, Bcr-AblT315I, Bcr-AblE255K, Bcr-AblG250E, Bcr-AblQ252H, Bcr-AblH396P, Bcr-AblM351T and Bcr-AblY253F, respectively. In a competitive binding assay, GZD824 bound to the ATP-binding sites of native Abl with Kd values of 0.32 and 0.34 nM for non-phosphorylated and phosphorylated Abl. In stably transformed Ba/F3 cells, GZD824 potently inhibited cells growth with IC50 values of 1.0 and 7.1 nM for Bcr-AblWT and Bcr-AblT315I expressed cells, respectively [1].
In mouse xenograft tumor models, GZD824 inhibited tumor growth. In mice bearing an allograft leukemia model, GZD824 significantly increased survival [1].
Reference:
Ren X, Pan X, Zhang Z, et al. Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib. J Med Chem, 2013, 56(3): 879-894.
| Cas No. | 1421783-64-3 | SDF | |
| 同義語 | GZD824 dimesylate; HQP1351 dimesylate | ||
| Chemical Name | 3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide dimethanesulfonate | ||
| Canonical SMILES | CC1=CC=C(C(NC2=CC=C(CN3CCN(C)CC3)C(C(F)(F)F)=C2)=O)C=C1C#CC4=CN=C5C(C=NN5)=C4.CS(=O)(O)=O.CS(=O)(O)=O | ||
| Formula | C29H27F3N6O.2CH4O3S | M.Wt | 724.77 |
| 溶解度 | ≥ 36.25mg/mL in DMSO | Storage | 4°C, away from moisture and light |
| 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 | 1.3797 mL | 6.8987 mL | 13.7975 mL |
| 5 mM | 0.2759 mL | 1.3797 mL | 2.7595 mL |
| 10 mM | 0.138 mL | 0.6899 mL | 1.3797 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)
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