| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| ln Vitro |
In an anti-proliferation experiment, CAN508 lowers the frequency of S-phase cells in the cancer cell line HT-29 [1]. In all three esophageal cancer cell lines (SKGT4, OE33, and FLO-1 cells), CAN508 (20–40 μM; 72 hours) dramatically inhibited cell growth in a dose-dependent manner, with an IC50 ranging from 34.99 to 91.09 μM[2]. All three kinds of esophageal cancer cell types exhibit increased apoptosis in response to CAN508 (40 μM; 72 hours) [2].
|
|---|---|
| ln Vivo |
On esophageal cancer xenografts, CAN508 (60 mg/kg; i.p.; once daily for 10 days) has antitumor activity [1].
|
| Cell Assay |
Apoptosis analysis[1]
Cell Types: SKGT4, OE33 and FLO-1 Cell Tested Concentrations: 40 μM Incubation Duration: 72 hrs (hours) Experimental Results: Increased apoptosis in all three esophageal adenocarcinoma cells compared to untreated controls 2 times. |
| Animal Protocol |
Animal/Disease Models: 4weeks old female nude mice (esophageal adenocarcinoma xenograft) [1]
Doses: 60 mg/kg Route of Administration: Ip; one time/day for 10 days Experimental Results: Tumor growth starting on the third day after treatment diminished by 50.83%. |
| References |
|
| Additional Infomation |
CAN-508 is a member of the class of pyrazoles that is 1H-pyrazole substituted by amino, (4-hydroxyphenyl)diazenyl, and amino groups at positions 3, 4 and 5, respectively. It is a CDK9 inhibitor (IC50 = 0.35 muM) with 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. It has a role as an angiogenesis inhibitor, an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of pyrazoles, a member of phenols, an aromatic amine and a monoazo compound.
|
| Molecular Formula |
C9H10N6O
|
|---|---|
| Molecular Weight |
218.22
|
| Exact Mass |
218.091
|
| CAS # |
140651-18-9
|
| PubChem CID |
135398514
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.7±0.1 g/cm3
|
| Boiling Point |
638.3±55.0 °C at 760 mmHg
|
| Flash Point |
339.8±31.5 °C
|
| Vapour Pressure |
0.0±2.0 mmHg at 25°C
|
| Index of Refraction |
1.803
|
| LogP |
0.4
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
16
|
| Complexity |
252
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=C(C=CC(=C1)O)N=NC2=C(N)NNC2=N
|
| InChi Key |
AYZRKFOEZQBUEA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H10N6O/c10-8-7(9(11)15-14-8)13-12-5-1-3-6(16)4-2-5/h1-4,16H,(H5,10,11,14,15)
|
| Chemical Name |
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol
|
| Synonyms |
CAY 10574; CAY-10574; CAY10574
|
| 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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~250 mg/mL (~1145.63 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5825 mL | 22.9127 mL | 45.8253 mL | |
| 5 mM | 0.9165 mL | 4.5825 mL | 9.1651 mL | |
| 10 mM | 0.4583 mL | 2.2913 mL | 4.5825 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
