Zotiraciclib (TG-02, SB-1317)

Alias: SB1317; Zotiraciclib; TG02
Cat No.:V7667 Purity: ≥98%
Zotiraciclib (formerly TG02, SB1317) isan orally bioavailable, brain penetrant and multi-kinase (CDK/JAK2/FLT3) inhibitor for the treatment of cancer (e.
Zotiraciclib (TG-02, SB-1317) Chemical Structure CAS No.: 1204918-72-8
Product category: CDK
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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Other Forms of Zotiraciclib (TG-02, SB-1317):

  • (E/Z)-Zotiraciclib ((E/Z)-TG02; (E/Z)-SB1317)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Zotiraciclib (formerly TG02, SB1317) is an orally bioavailable, brain penetrant and multi-kinase (CDK/JAK2/FLT3) inhibitor for the treatment of cancer (e.g. anaplastic astrocytoma and GBM, as well as DIPG, a rare pediatric cance). In Singapore, S*BIO Pte Ltd made the discovery of this small molecule macrocyclic compound. By inhibiting cyclin-dependent kinase 9 (CDK9), it depletes Myc and passes through the blood-brain barrier (BBB). It is one of several CDK inhibitors being studied for the treatment of cancer; other CDK inhibitors that target CDK9 for the treatment of acute myeloid leukemia (AML) include atuveciclib and alvocidib. Eighty percent of glioblastomas exhibit this feature, which is indicative of myc overexpression, a factor known to be involved in a variety of cancers. The US Food and Drug Administration (FDA) and the European Medicines Agency (EMA) have designated zotiraciclib as an orphan drug for the treatment of gliomas.

Biological Activity I Assay Protocols (From Reference)
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H24N4O
Molecular Weight
372.462864875793
Exact Mass
372.1950114
CAS #
1204918-72-8
SMILES
CN1C/C=C/CCOC2=CC=CC(=C2)C3=NC(=NC=C3)NC4=CC=CC(=C4)C1
InChi Key
VXBAJLGYBMTJCY-NSCUHMNNSA-N
InChi Code
InChI=1S/C23H24N4O/c1-27-13-3-2-4-14-28-21-10-6-8-19(16-21)22-11-12-24-23(26-22)25-20-9-5-7-18(15-20)17-27/h2-3,5-12,15-16H,4,13-14,17H2,1H3,(H,24,25,26)/b3-2+
Chemical Name
(16E)-14-methyl-20-oxa-5,7,14,27-tetrazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2(27),3,5,8,10,12(26),16,21,23-decaene
Synonyms
SB1317; Zotiraciclib; TG02
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~50 mg/mL (~134.2 mM)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05588141 Recruiting Drug: Zotiraciclib Brain Tumor
Cancer
National Cancer Institute
(NCI)
May 16, 2023 Phase 1
Phase 2
NCT02942264 Completed Drug: Zotiraciclib
(TG02)
Drug: Temozolomide
(TMZ)
Brain Tumor
Astrocytoma
National Cancer Institute
(NCI)
December 14, 2016 Phase 1
Phase 2
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