| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| Targets |
CDK2 13 nM (IC50) JAK2 73 nM (IC50) FLT3 56 nM (IC50)
|
|---|---|
| ln Vitro |
(E/Z)-Zotiraciclib (0-10 μM) demonstrates strong inhibition of FLT3, JAK2, and CDK2, with IC50 values of 13, 73, and 56 nM, respectively[1]. Cancer cell growth is inhibited by (E/Z)-Zotiraciclib (0–10 μM; 48 h)[1]. At an IC50 value of 0.13 μM, (E/Z)-Zotiraciclib (8-1000 nM; 24 h) potently suppresses the CDK2 biomarker pRb in HCT-116 cells and potently opposes pRb in MV4-11 cells[1].
|
| ln Vivo |
(E/Z)-Zotiraciclib (50 and 75 mg/kg; po once daily for 3 weeks) suppresses the growth of tumors[1]. Zotiraciclib (E/Z) (15 and 75 mg/kg; po once daily for two days on and five days off; ip once daily for five days on and five days off) suppresses the growth of tumors in two ways[1].
|
| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: HL-60, HCT-116, RAMOS, COLO205 and DU145 cell lines Tested Concentrations: 0-10 μM Incubation Duration: 48 h Experimental Results: 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. |
| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse: with HCT-116 colon cancer cells xenografts[1]
Doses: 50 and 75 mg/kg Route of Administration: po (oral gavage); 50 and 75 mg/kg one time/day for 3 weeks Experimental Results: Dramatically inhibited the growth of tumors with a mean TGI of 82 %. Animal/Disease Models: Male balb/c (Bagg ALBino) mouse: with lymphoma Ramos cells xenografts[1] Doses: 15 and 75 mg/kg Route of Administration: po (oral gavage) and intraperitoneal (ip)injection; 75 mg/kg one time/day 2 days on and 5 days off (po) and 15 mg/kg one time/day 5 days on 5 days off (ip) Experimental Results: Dramatically inhibited the growth of tumors with mean TGIs of 42% and 63% for the oral and ip delivery methods, respectively. |
| 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 |
372.46
|
| Exact Mass |
372.195
|
| CAS # |
937270-47-8
|
| Related CAS # |
(E/Z)-Zotiraciclib hydrochloride;1321626-25-8;Zotiraciclib;1204918-72-8
|
| PubChem CID |
16739650
|
| Appearance |
Off-white to light yellow solid powder
|
| 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 |
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
|
| 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 : 26.5 mg/mL (71.15 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.58 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 20.8 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: ≥ 2.08 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
