| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
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.
| References |
|
|---|---|
| Additional Infomation |
Zotiraciclib is under investigation in clinical trial NCT02942264 (Zotiraciclib (TG02) Plus Dose-dense or Metronomic Temozolomide Followed by Randomized Phase II Trial of Zotiraciclib (TG02) Plus Temozolomide Versus Temozolomide Alone in Adults With Recurrent Anaplastic Astrocytoma and Glioblastoma).
|
| Molecular Formula |
C23H24N4O
|
|---|---|
| Molecular Weight |
372.462864875793
|
| Exact Mass |
372.195
|
| CAS # |
1204918-72-8
|
| Related CAS # |
(E/Z)-Zotiraciclib;937270-47-8
|
| PubChem CID |
16739650
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
577.1±60.0 °C at 760 mmHg
|
| Flash Point |
302.8±32.9 °C
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
| Index of Refraction |
1.577
|
| LogP |
4.76
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
28
|
| Complexity |
499
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CN1CC=CCCOC2=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
|
| HS Tariff Code |
2934.99.9001
|
| 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 (In Vitro) |
DMSO: ~50 mg/mL (~134.2 mM）
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.71 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
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.
| 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 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA