Olverembatinib dimesylate
Based on 10 publication(s) in Google Scholar
Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-AblT315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity. Olverembatinib (dimesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Reinheit: 99.80%
- CAS. Nr.: 1421783-64-3
- Formel: C31H35F3N6O7S2
- Molecular Weight:724.77
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Speicherung:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Olverembatinib dimesylate
More- Cancer Res. 2025 Jan 2;85(1):101-117. [Abstract]
- J Exp Clin Cancer Res. 2025 Jul 8;44(1):195. [Abstract]
- Free Radic Biol Med. 2025 Sep 19:S0891-5849(25)00942-6. [Abstract]
- Sci Data. 2024 Sep 19;11(1):1024. [Abstract]
- Sci Rep. 2026 Feb 8;16(1):7792. [Abstract]
- Biochim Biophys Acta. 2018 May 25;1865(9):1173-1186. [Abstract]
- Exp Cell Res. 2026 Feb 1;455(1):114851. [Abstract]
- bioRxiv. 2025 August 23.
- Research Square Print. 2023 Mar 23.
- Research Square Preprint. 2021 Oct.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Cell Proliferation/Viability Assay
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Apoptosis Analysis
Biologische Aktivität
IC50: 0.68 nM (Bcr-AblT315I), 0.27 nM (Bcr-AblE255K) , 0.71 nM (Bcr-AblG250E) , 0.15 nM (Bcr-AblQ252H), 0.35 nM (Bcr-Abl H396P), 0.29 nM (Bcr-Abl M351T), 0.35 nM (Bcr-AblY253F), Bcr-AblF317L[1]
Olverembatinib dimesylate shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants[1].
Olverembatinib dimesylate selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells[1].
Olverembatinib dimesylate 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells
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Concentration:1 nM, 2 nM, 5 nM, 10 nM, 20nM
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Incubation Time:4.0 hours
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Result:Inhibited Bcr-Abl signaling in K562 cell lines.
Olverembatinib dimesylate (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].
Olverembatinib dimesylate exhibits a good oral bioavailability (rat 48.7%) and Cmax (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg)[1].
Olverembatinib dimesylate 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID nude mice, bearing allografted Ba/F3 cells expressing Bcr-AblT315I[1]
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Dosage:1 mg/kg, 2 mg/kg, 5.0 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:Oral gavage, daily, for 10 days
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Result:Efficiently prolonged animal survival in an allograft leukemia tumor model.
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Animal Model:Rats[1]
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Dosage:5 mg/kg for i.v.; 25 mg/kg for oral (Pharmacokinetic Analysis)
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Administration:Intravenous injection and oral administration
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Result:Oral bioavailability (48.7%), Cmax (390.5 μg/L), T1/2 (5.6 h).
Chemical Information
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CAS. Nr. 1421783-64-3
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Appearance Solid
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Molecular Weight 724.77
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Formel C31H35F3N6O7S2
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CC=C(C)C(C#CC4=CN=C(NN=C5)C5=C4)=C3.CS(=O)(O)=O.CS(=O)(O)=O
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Synonyms
GZD824 dimesylate; HQP1351 dimesylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (10)
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Journal Impact Factor
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Most Recent
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Cancer Res
Targeted Degradation of SOS1 Exhibits Potent Anticancer Activity and Overcomes Resistance in KRAS-Mutant Tumors and BCR-ABL-Positive Leukemia. [Abstract]2025 Jan 2;85(1):101-117. PMID: 39437162
Olverembatinib dimesylate purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jan 2;85(1):101-117. [Abstract]
Cell apoptosis (Annexin V+) of the K562 and KU812 cells treated with SIAIS562055, TKIs such as imatinib, nilotinib, or Olverembatinib (olvere, 1 nM), alone or in combination, for 48 hours.
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J Exp Clin Cancer Res
Genomic profiling of a collection of patient-derived xenografts and cell lines identified ixabepilone as an active drug against chemo-resistant osteosarcoma. [Abstract]2025 Jul 8;44(1):195. PMID: 40624718
Olverembatinib dimesylate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 8;44(1):195. [Abstract]
Dose-response curves of PDX-OS#29-C treated with a titration of Olverembatinib for 96 h were generated.
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Free Radic Biol Med
ENO1 blockade augment ferroptosis susceptibility in TKIs-resistant CML through GPX4 autophagic degradation. [Abstract]2025 Sep 19:S0891-5849(25)00942-6. PMID: 40976411 -
Sci Data
High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]2024 Sep 19;11(1):1024. PMID: 39300112 -
Sci Rep
A novel human acute myeloid leukemia cell line SDEY-AML1 with KMT2A: MLLT3, IKZF1: EVX1 fusions exhibits high tumorigenicity in NSG mice. [Abstract]2026 Feb 8;16(1):7792. PMID: 41656387 -
Biochim Biophys Acta
c-Abl phosphorylation of Yin Yang 1's conserved tyrosine 254 in the spacer region modulates its transcriptional activity. [Abstract]2018 May 25;1865(9):1173-1186. PMID: 29807053
Olverembatinib dimesylate purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta. 2018 May 25;1865(9):1173-1186. [Abstract]
Cell lysates are prepared from HCT-116 cells transfected with Flag-Vector or Flag-YY1. Twenty-four hours following transfection cells are treated with Olverembatinib (GZD824) with the indicated concentration for 4 h prior to 200 μM Pervanadate treatment for 30 min. Lysates are subjected to immunoprecipitation using α-Flag M2 resin followed by Western blotting.
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Exp Cell Res
Overcoming multidrug resistance in cancer cells targeting ABC transporter ABCB1 with tyrosine kinase inhibitor: Olverembatinib. [Abstract]2026 Feb 1;455(1):114851. PMID: 41386459
Olverembatinib dimesylate purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2026 Feb 1;455(1):114851. [Abstract]
The cytotoxicity of Olverembatinib (0.1-10 μM; 72 h) was observed in different cells.
Olverembatinib dimesylate purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2026 Feb 1;455(1):114851. [Abstract]
The effect of Olverembatinib (0.03-0.3 μM; 120 min) on the accumulation of Rhodamine 123 in KB-3-1 and KB-C2 cells.
Olverembatinib dimesylate purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2026 Feb 1;455(1):114851. [Abstract]
Olverembatinib (5-10 μM; 3 min) increased the ATPase of ABCB1 at lower concentration.
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Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (172.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (68.99 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (2.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (2.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (394 KB)
- English - EN (394 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.3797 mL | 6.8987 mL | 13.7975 mL | 34.4937 mL |
| 5 mM | 0.2759 mL | 1.3797 mL | 2.7595 mL | 6.8987 mL | |
| 10 mM | 0.1380 mL | 0.6899 mL | 1.3797 mL | 3.4494 mL | |
| 15 mM | 0.0920 mL | 0.4599 mL | 0.9198 mL | 2.2996 mL | |
| 20 mM | 0.0690 mL | 0.3449 mL | 0.6899 mL | 1.7247 mL | |
| 25 mM | 0.0552 mL | 0.2759 mL | 0.5519 mL | 1.3797 mL | |
| 30 mM | 0.0460 mL | 0.2300 mL | 0.4599 mL | 1.1498 mL | |
| 40 mM | 0.0345 mL | 0.1725 mL | 0.3449 mL | 0.8623 mL | |
| 50 mM | 0.0276 mL | 0.1380 mL | 0.2759 mL | 0.6899 mL | |
| 60 mM | 0.0230 mL | 0.1150 mL | 0.2300 mL | 0.5749 mL | |
| DMSO | 80 mM | 0.0172 mL | 0.0862 mL | 0.1725 mL | 0.4312 mL |
| 100 mM | 0.0138 mL | 0.0690 mL | 0.1380 mL | 0.3449 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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