(E/Z)-Zotiraciclib hydrochloride
Based on 6 publication(s) in Google Scholar
(E/Z)-Zotiraciclib ((E/Z)-TG02) is an orally active inhibitor of CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively. (E/Z)-Zotiraciclib effectively inhibits the proliferation of cancer cells, it can be used for the research of cancer.
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- Pureza: 99.90%
- No. CAS: 1321626-25-8
- Fòrmula: C23H25ClN4O
- Peso molecular:408.92
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) (E/Z)-Zotiraciclib hydrochloride
More- Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
- Adv Sci (Weinh). 2025 Feb;12(7):e2413514. [Abstract]
- Mol Cancer Res. 2020 Oct;18(10):1512-1521. [Abstract]
- Cancers (Basel). 2022 Mar 19;14(6):1575. [Abstract]
- ACS Chem Biol. 2016 Jun 17;11(6):1710-9. [Abstract]
- J Neurosurg Pediatr. 2021 Sep 3;28(6):734-743. [Abstract]
Actividad biológica
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CDK2 |
JAK2 |
FLT3 |
(E/Z)-Zotiraciclib (0-10 μM) hydrochloride shows potent inhibition to CDK2, JAK2 and FLT3 with IC50s of 13, 73 and 56 nM, respectively[1]. (E/Z)-Zotiraciclib (0-10 μM; 48 h) hydrochloride inhibits proliferation of cancer cells[1]. (E/Z)-Zotiraciclib (8-1000 nM; 24 h) hydrochloride potently inhibits the CDK2 biomarker pRb in HCT-116 cells and potently againsts pRb in MV4-11 cells with an IC50 value of 0.13 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HL-60, HCT-116, RAMOS, COLO205 and DU145 cell lines
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Concentration:up to 10 μM
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Incubation Time:48 h
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Result:Inhibited proliferation of HL-60, HCT-116, RAMOS, COLO205 and DU145 cells with IC50s of 0.059, 0.079, 0.033, 0.072 and 0.14 μM, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male BALB/c mice with HCT-116 colon cancer cells xenografts[1]
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Dosage:50 and 75 mg/kg
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Administration:Oral gavage; 50 and 75 mg/kg once daily for 3 weeks
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Result:Significantly inhibited the growth of tumors with a mean TGI of 82%.
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Animal Model:BALB/c mice with lymphoma Ramos cells xenografts[1]
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Dosage:15 and 75 mg/kg
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Administration:Oral gavage and intraperitoneal injection ; 75 mg/kg once daily 2 days on and 5 days off (p.o.) and 15 mg/kg once daily 5 days on 5 days off (i.p.)
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Result:Significantly inhibited the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively.
Chemical Information
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No. CAS 1321626-25-8
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Appearance Solid
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Peso molecular 408.92
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Fòrmula C23H25ClN4O
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Color White to light yellow
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SMILES
CN1CC2=CC(NC3=NC(C4=CC(OCC/C=C/C1)=CC=C4)=CC=N3)=CC=C2.Cl
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Synonyms
(E/Z)-TG02 hydrochloride; (E/Z)-SB1317 hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (6)
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Journal Impact Factor
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Most Recent
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Science
2017 Dec 1;358(6367):eaan4368. PMID: 29191878 -
Adv Sci (Weinh)
Targeting CDK2 Confers Vulnerability to Lenvatinib Via Driving Senescence in Anaplastic Thyroid Cancer. [Abstract]2025 Feb;12(7):e2413514. PMID: 39716890 -
Mol Cancer Res
2020 Oct;18(10):1512-1521. PMID: 32611550 -
Cancers (Basel)
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening. [Abstract]2022 Mar 19;14(6):1575. PMID: 35326726 -
ACS Chem Biol
Conformational Adaption May Explain the Slow Dissociation Kinetics of Roniciclib (BAY 1000394), a Type I CDK Inhibitor with Kinetic Selectivity for CDK2 and CDK9. [Abstract]2016 Jun 17;11(6):1710-9. PMID: 27090615 -
J Neurosurg Pediatr
Targeting of cyclin-dependent kinases in atypical teratoid rhabdoid tumors with multikinase inhibitor TG02. [Abstract]2021 Sep 3;28(6):734-743. PMID: 34479190
Solvente y solubilidad
DMSO : 33.33 mg/mL (81.51 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (6.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.11 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. William AD, et al. Discovery of kinase spectrum selective macrocycle (16E)-14-methyl-20-oxa-5,7,14,26-tetraazatetracyclo[19.3.1.1(2,6).1(8,12)]heptacosa-1(25),2(26),3,5,8(27),9,11,16,21,23-decaene (SB1317/TG02), a potent inhibitor of cyclin dependent kinases (CDKs), Janus kinase 2 (JAK2), and fms-like tyrosine kinase-3 (FLT3) for the treatment of cancer. J Med Chem. 2012;55(1):169-196. [Content Brief]
[2]. Pasha MK, et al. Preclinical metabolism and pharmacokinetics of SB1317 (TG02), a potent CDK/JAK2/FLT3 inhibitor. Drug Metab Lett. 2012 Mar;6(1):33-42. [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). 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 |
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| DMSO | 1 mM | 2.4455 mL | 12.2273 mL | 24.4547 mL | 61.1367 mL |
| 5 mM | 0.4891 mL | 2.4455 mL | 4.8909 mL | 12.2273 mL | |
| 10 mM | 0.2445 mL | 1.2227 mL | 2.4455 mL | 6.1137 mL | |
| 15 mM | 0.1630 mL | 0.8152 mL | 1.6303 mL | 4.0758 mL | |
| 20 mM | 0.1223 mL | 0.6114 mL | 1.2227 mL | 3.0568 mL | |
| 25 mM | 0.0978 mL | 0.4891 mL | 0.9782 mL | 2.4455 mL | |
| 30 mM | 0.0815 mL | 0.4076 mL | 0.8152 mL | 2.0379 mL | |
| 40 mM | 0.0611 mL | 0.3057 mL | 0.6114 mL | 1.5284 mL | |
| 50 mM | 0.0489 mL | 0.2445 mL | 0.4891 mL | 1.2227 mL | |
| 60 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0189 mL | |
| 80 mM | 0.0306 mL | 0.1528 mL | 0.3057 mL | 0.7642 mL |
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