2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK JAK/STAT Signaling Epigenetics Stem Cell/Wnt
  3. CDK JAK FLT3
  4. (E/Z)-Zotiraciclib

(E/Z)-Zotiraciclib  (Synonyms: (E/Z)-TG02; (E/Z)-SB1317)

Cat. No.: HY-15166 Purity: 99.70%
COA Handling Instructions

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(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.

For research use only. We do not sell to patients.

(E/Z)-Zotiraciclib Chemical Structure

(E/Z)-Zotiraciclib Chemical Structure

CAS No. : 937270-47-8

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10 mM * 1 mL in DMSO
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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of (E/Z)-Zotiraciclib:

(E/Z)-Zotiraciclib Related Antibodies

Top Publications Citing Use of Products

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

(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[1][2].

IC50 & Target[1]

CDK2

13 nM (IC50)

JAK2

73 nM (IC50)

FLT3

56 nM (IC50)

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.

(E/Z)-Zotiraciclib Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HL-60, HCT-116, RAMOS, COLO205 and DU145 cell lines
Concentration: 0-10 μM
Incubation Time: 48 h
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

(E/Z)-Zotiraciclib (50 and 75 mg/kg; p.o. once daily for 3 weeks) inhibits tumor growth[1].
? (E/Z)-Zotiraciclib (15 and 75 mg/kg; p.o. once daily 2 days on and 5 days off; i.p. once daily 5 days on 5 days off) inhibits tumor growth in two manners[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c mice with HCT-116 colon cancer cells xenografts[1]
Dosage: 50 and 75 mg/kg
Administration: Oral gavage; 50 and 75 mg/kg once daily for 3 weeks
Result: Significantly inhibited the growth of tumors with a mean TGI of 82%.
Animal Model: Male BALB/c mice with lymphoma Ramos cells xenografts[1]
Dosage: 15 and 75 mg/kg
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.)
Result: Significantly inhibited the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively.
Molecular Weight

372.46

Formula

C23H24N4O
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CN1CC2=CC(NC3=NC(C4=CC(OCC/C=C/C1)=CC=C4)=CC=N3)=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6849 mL 13.4243 mL 26.8485 mL
5 mM 0.5370 mL 2.6849 mL 5.3697 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.96%

COA (255 KB) HNMR (211 KB) LCMS (121 KB)

Handling Instructions (2659 KB)
References

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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(E/Z)-Zotiraciclib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

(E/Z)-Zotiraciclib937270-47-8(E/Z)-TG02 (E/Z)-SB1317CDKJAKFLT3Cyclin dependent kinaseJanus kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3anti-cancerproliferationpRbbiomarkerHCT-116MV4-11micetumorxenograftInhibitorinhibitorinhibit

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