Olverembatinib (Synonyms: GZD824; HQP1351) |
カタログ番号GC62207
One-Click Copy Product Info
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オルベレンマチニブ (GZD824) は、経口で有効な強力な汎 Bcr-Abl 阻害剤です。オルベレンマチニブは、広範囲の Bcr-Abl 変異体を強力に阻害します。オルベレンマチニブは、天然の Bcr-Abl および Bcr-AblT315I をそれぞれ 0.34 nM および 0.68 nM の IC50 で強力に阻害します。オルベレンマチニブ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.: 1257628-77-5
Sample solution is provided at 25 µL, 10mM.
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GZD824 (HQP1351) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity[1].
GZD824 shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants[1].GZD824 selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells[1].GZD824 inhibits Bcr-Abl signaling in K562 (1-20 nM; 4.0 hours) and Ba/F3 stable cell lines expressing native Bcr-Abl (0.1-100 nM; 4.0 hours) or Bcr-AblT315I(0.1-100 nM; 4.0 hours)[1].
GZD824 suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl WT[1].GZD824 (1-20 mg/kg; i.g.; daily; for 10 days) significantly increases the median survival of the mice bearing allografted Ba/F3 cells expressing Bcr-AblT315I[1].GZD824 exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg)[1].GZD824 exhibits terminal elimination half-lives (rat 5.6 h) due to high plasma clearance (rat 1.7 L/h/kg) following intravenous administration (rat 5 mg/kg)[1].
[1]. Ren X, Pan X, Zhang Z, 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 Feb 14;56(3):879-94.
| Cas No. | 1257628-77-5 | SDF | |
| 同義語 | GZD824; HQP1351 | ||
| Formula | C29H27F3N6O | M.Wt | 532.56 |
| 溶解度 | DMSO : ≥ 100 mg/mL (187.77 mM) | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8777 mL | 9.3886 mL | 18.7772 mL |
| 5 mM | 375.5 μL | 1.8777 mL | 3.7554 mL |
| 10 mM | 187.8 μL | 938.9 μL | 1.8777 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 saline, 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)