| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
CAY10574 selectively targets CDK9, a kinase that regulates transcriptional elongation by phosphorylating RNA polymerase II. It shows 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. It also acts as a competitive inhibitor of Cdk2-cyclin E with respect to ATP.
|
|---|---|
| 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].
In vitro, CAY10574 is a potent, ATP-competitive inhibitor of CDK9/cyclin T1. It exhibits an IC50 of 0.35 µM for CDK9 and is 38 times more selective for CDK9/cyclin T1 than other CDK/cyclins. It has anti-tumor effects. |
| ln Vivo |
On esophageal cancer xenografts, CAN508 (60 mg/kg; i.p.; once daily for 10 days) has antitumor activity [1].
In vivo, the anti-tumor effects of CAY10574 have been demonstrated in preclinical models. By inhibiting CDK9, it reduces the transcription of short-lived anti-apoptotic proteins, thereby inducing apoptosis in cancer cells. |
| Enzyme Assay |
The in vitro enzyme assay measures the inhibition of CDK9 kinase activity. This is typically performed using a radioactive or luminescent assay where the kinase is incubated with a substrate peptide and ATP in the presence of the inhibitor, and the incorporation of phosphate is measured.
|
| 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. In vitro cell-based assays are performed in cancer cell lines. Cells are treated with CAY10574, and the effect on cell proliferation is measured. The inhibition of CDK9 is confirmed by assessing the phosphorylation of RNA polymerase II and the expression of its target genes, such as Mcl-1. |
| 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%. In vivo activity is evaluated in mouse xenograft models of cancer. Tumor-bearing mice are treated with CAY10574, and tumor growth is monitored. The induction of apoptosis and inhibition of proliferation in tumor tissue is confirmed by histological analysis. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of CAY10574 are not detailed in the literature. As a research compound, its primary use is in vitro, and its in vivo PK properties would need to be determined for any therapeutic development.
|
| Toxicity/Toxicokinetics |
Toxicological data for CAY10574 is not available. As a research compound, it is not intended for human use. Its safety profile would need to be established if it were to be developed further.
|
| References |
|
| Additional Infomation |
CAN-508 is a pyrazole compound with the structure 1H-pyrazole, substituted at positions 3, 4, and 5 with amino, (4-hydroxyphenyl)diazo, and amino groups, respectively. It is a CDK9 inhibitor (IC50 = 0.35 μM) with 38-fold higher selectivity for the CDK9/cyclin T complex than other CDK/cyclin complexes. It exhibits a variety of activities, including angiogenesis inhibition, EC 2.7.11.22 (cyclin-dependent kinase) inhibition, antitumor activity, and apoptosis induction. CAN-508 belongs to the pyrazole, phenol, aromatic amine, and monoazo compound classes.
CAY10574 is a valuable research tool for studying the role of CDK9 in transcription and cancer. Its high selectivity makes it a useful compound for dissecting the specific functions of CDK9. It is not an approved drug. |
| Molecular Formula |
C9H10N6O
|
|---|---|
| Molecular Weight |
218.22
|
| Exact Mass |
218.091
|
| CAS # |
140651-18-9
|
| PubChem CID |
135398514
|
| Appearance |
Light yellow to yellow solid powder
|
| 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
