(E/Z)-Zotiraciclib
Based on 6 publication(s) in Google Scholar
(E/Z)-Zotiraciclib ((E/Z)-TG02) is a potent 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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 99.70%
- CAS No.: 937270-47-8
- Formule: C23H24N4O
- Masse moléculaire:372.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) (E/Z)-Zotiraciclib
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]
Activité biologique
Description
IC50 & Target
[1]|
CDK2 13 nM (IC50) |
JAK2 73 nM (IC50) |
FLT3 56 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COLO 205 | IC50 |
0.072 μM
Compound: 26h, SB1317/TG02
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Antiproliferative activity against human COLO205 cells after 48 hrs
Antiproliferative activity against human COLO205 cells after 48 hrs
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[PMID: 22148278] |
| DU-145 | IC50 |
0.14 μM
Compound: 26h, SB1317/TG02
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Antiproliferative activity against human DU145 cells after 48 hrs
Antiproliferative activity against human DU145 cells after 48 hrs
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[PMID: 22148278] |
| HCT-116 | IC50 |
0.079 μM
Compound: 26h, SB1317/TG02
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Antiproliferative activity against human HCT116 cells after 48 hrs
Antiproliferative activity against human HCT116 cells after 48 hrs
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[PMID: 22148278] |
| HEL | GI50 |
0.79 μM
Compound: SB1317
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Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay
Antiproliferative activity against human HEL cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay
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[PMID: 25800646] |
| HL-60 | GI50 |
1.13 μM
Compound: SB1317
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Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay
Antiproliferative activity against human HL60 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay
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[PMID: 25800646] |
| HL-60 | IC50 |
0.059 μM
Compound: 26h, SB1317/TG02
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Antiproliferative activity against human HL60 cells after 48 hrs
Antiproliferative activity against human HL60 cells after 48 hrs
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[PMID: 22148278] |
| K562 | GI50 |
1.23 μM
Compound: SB1317
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Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay
Antiproliferative activity against human K562 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay
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[PMID: 25800646] |
| MV4-11 | GI50 |
0.66 μM
Compound: SB1317
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Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay
Antiproliferative activity against human MV4-11 cells assessed as growth inhibition after 48 hrs by CellTiter-Glo assay
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[PMID: 25800646] |
| MV4-11 | IC50 |
0.13 μM
Compound: 26h, SB1317/TG02
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Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis
Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis
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[PMID: 22148278] |
| Ramos | IC50 |
0.033 μM
Compound: 26h, SB1317/TG02
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Antiproliferative activity against human Ramos cells after 48 hrs
Antiproliferative activity against human Ramos cells after 48 hrs
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[PMID: 22148278] |
| Sf21 | IC50 |
37 nM
Compound: TG02
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Inhibition of recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as subs
Inhibition of recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as subs
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[PMID: 30543440] |
| Sf21 | IC50 |
8 nM
Compound: TG02
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Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate
Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate
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[PMID: 30543440] |
In Vitro
(E/Z)-Zotiraciclib (0-10 μM) 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) inhibits proliferation of cancer cells[1]. (E/Z)-Zotiraciclib (8-1000 nM; 24 h) 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:0-10 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.
In Vivo
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:Male 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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CAS No. 937270-47-8
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Appearance Solid
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Masse moléculaire 372.46
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Formule C23H24N4O
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Color Off-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
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Synonyms
(E/Z)-TG02; (E/Z)-SB1317
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
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
Solvant et solubilité
In Vitro:
DMSO : 26.5 mg/mL (71.15 mM; Need ultrasonic and warming; 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (5.58 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 (5.58 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.
In Vivo Dissolution Calculator
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.
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[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 kina [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6849 mL | 13.4243 mL | 26.8485 mL | 67.1213 mL |
| 5 mM | 0.5370 mL | 2.6849 mL | 5.3697 mL | 13.4243 mL | |
| 10 mM | 0.2685 mL | 1.3424 mL | 2.6849 mL | 6.7121 mL | |
| 15 mM | 0.1790 mL | 0.8950 mL | 1.7899 mL | 4.4748 mL | |
| 20 mM | 0.1342 mL | 0.6712 mL | 1.3424 mL | 3.3561 mL | |
| 25 mM | 0.1074 mL | 0.5370 mL | 1.0739 mL | 2.6849 mL | |
| 30 mM | 0.0895 mL | 0.4475 mL | 0.8950 mL | 2.2374 mL | |
| 40 mM | 0.0671 mL | 0.3356 mL | 0.6712 mL | 1.6780 mL | |
| 50 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3424 mL | |
| 60 mM | 0.0447 mL | 0.2237 mL | 0.4475 mL | 1.1187 mL |
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