Zotiraciclib (Synonyms: TG02; SB1317)

Cat. No.: HY-15163: FAQs
Data Sheet Handling Instructions

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Zotiraciclib (TG02) is an orally active potent inhibitor of CDK2, JAK2 and FLT3 with IC₅₀ values of 13, 73, and 56 nM, respectively. Zotiraciclib can be used for the research of advanced leukemias and multiple myeloma.

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

Zotiraciclib Chemical Structure

CAS No. : 1204918-72-8

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Other Forms of Zotiraciclib:

(E/Z)-Zotiraciclib In-stock
Zotiraciclib hydrochloride Get quote

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•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

View All Isoforms

JAK1 JAK2 JAK3 Tyk2 JAK

View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Purity & Documentation
References
Customer Review

Description

Molecular Weight

372.46

Formula

C₂₃H₂₄N₄O

CAS No.

1204918-72-8

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

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (134.24 mM; Need ultrasonic; 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
10 mM	0.2685 mL	1.3424 mL	2.6849 mL

View the Complete Stock Solution Preparation Table

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.71 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.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Handling Instructions (2659 KB)

References

[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 Jan 12;55(1):169-96. [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

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
	80 mM	0.0336 mL	0.1678 mL	0.3356 mL	0.8390 mL
	100 mM	0.0268 mL	0.1342 mL	0.2685 mL	0.6712 mL

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.

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