CAN508
Based on 1 publication(s) in Google Scholar
CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.71%
- No. CAS: 140651-18-9
- Fòrmula: C9H10N6O
- Peso molecular:218.22
-
Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) CAN508
More
Actividad biológica
|
CDK9/cyclinT1 0.35 μM (IC50) |
CDK2/cyclinE 20 μM (IC50) |
cdk2/cyclin A 69 μM (IC50) |
Cdk4/cyclin D1 13.5 μM (IC50) |
CDK7/cyclin H 26 μM (IC50) |
Cdk1/cyclin B 44 μM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 786-0 | GI50 |
26.2 μM
Compound: CAN508
|
Cytotoxicity against human 786-0 cells
Cytotoxicity against human 786-0 cells
|
[PMID: 21777997] |
| A498 | GI50 |
18.2 μM
Compound: CAN508
|
Cytotoxicity against human A498 cells
Cytotoxicity against human A498 cells
|
[PMID: 21777997] |
| A549 | GI50 |
22.5 μM
Compound: CAN508
|
Cytotoxicity against human A549 cells
Cytotoxicity against human A549 cells
|
[PMID: 21777997] |
| ACHN | GI50 |
15.6 μM
Compound: CAN508
|
Cytotoxicity against human ACHN cells
Cytotoxicity against human ACHN cells
|
[PMID: 21777997] |
| BT-549 | GI50 |
14 μM
Compound: CAN508
|
Cytotoxicity against human BT549 cells
Cytotoxicity against human BT549 cells
|
[PMID: 21777997] |
| CAKI-1 | GI50 |
14.8 μM
Compound: CAN508
|
Cytotoxicity against human Caki1 cells
Cytotoxicity against human Caki1 cells
|
[PMID: 21777997] |
| CCRF-CEM | GI50 |
20 μM
Compound: CAN508
|
Cytotoxicity against human CCRF-CEM cells
Cytotoxicity against human CCRF-CEM cells
|
[PMID: 21777997] |
| COLO 205 | GI50 |
18.9 μM
Compound: CAN508
|
Cytotoxicity against human COLO205 cells
Cytotoxicity against human COLO205 cells
|
[PMID: 21777997] |
| DU-145 | GI50 |
17 μM
Compound: CAN508
|
Cytotoxicity against human DU145 cells
Cytotoxicity against human DU145 cells
|
[PMID: 21777997] |
| EKVX | GI50 |
22 μM
Compound: CAN508
|
Cytotoxicity against human EKVX cells
Cytotoxicity against human EKVX cells
|
[PMID: 21777997] |
| G-361 | IC50 |
64 μM
Compound: 31b, (CAN508)
|
Antiproliferative activity against G361 cell line
Antiproliferative activity against G361 cell line
|
[PMID: 17064068] |
| HCC 2998 | GI50 |
29.4 μM
Compound: CAN508
|
Cytotoxicity against human HCC2998 cells
Cytotoxicity against human HCC2998 cells
|
[PMID: 21777997] |
| HCT-116 | GI50 |
18.9 μM
Compound: CAN508
|
Cytotoxicity against human HCT116 cells
Cytotoxicity against human HCT116 cells
|
[PMID: 21777997] |
| HCT-15 | GI50 |
24.2 μM
Compound: CAN508
|
Cytotoxicity against human HCT15 cells
Cytotoxicity against human HCT15 cells
|
[PMID: 21777997] |
| HL-60(TB) | GI50 |
6.4 μM
Compound: CAN508
|
Cytotoxicity against human HL-60(TB) cells
Cytotoxicity against human HL-60(TB) cells
|
[PMID: 21777997] |
| HMEC-1 | IC50 |
20 μM
Compound: CAN508
|
Inhibition of RNA synthesis in human HMEC1 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting
Inhibition of RNA synthesis in human HMEC1 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting
|
[PMID: 21777997] |
| HOP-62 | GI50 |
31.8 μM
Compound: CAN508
|
Cytotoxicity against human HOP62 cells
Cytotoxicity against human HOP62 cells
|
[PMID: 21777997] |
| HOP-92 | GI50 |
18.2 μM
Compound: CAN508
|
Cytotoxicity against human HOP92 cells
Cytotoxicity against human HOP92 cells
|
[PMID: 21777997] |
| HOS | IC50 |
49 μM
Compound: 31b, (CAN508)
|
Antiproliferative activity against HOS cell line
Antiproliferative activity against HOS cell line
|
[PMID: 17064068] |
| Hs-578T | GI50 |
21.8 μM
Compound: CAN508
|
Cytotoxicity against human Hs 578T cells
Cytotoxicity against human Hs 578T cells
|
[PMID: 21777997] |
| HT-29 | GI50 |
29.7 μM
Compound: CAN508
|
Cytotoxicity against human HT-29 cells
Cytotoxicity against human HT-29 cells
|
[PMID: 21777997] |
| IGROV-1 | GI50 |
20.6 μM
Compound: CAN508
|
Cytotoxicity against human IGROV1 cells
Cytotoxicity against human IGROV1 cells
|
[PMID: 21777997] |
| K562 | GI50 |
9.2 μM
Compound: CAN508
|
Cytotoxicity against human K562 cells
Cytotoxicity against human K562 cells
|
[PMID: 21777997] |
| K562 | IC50 |
33 μM
Compound: IIIa, CAN508
|
Cytotoxicity against human K562 cells after 72 hrs by calcein AM staining-based fluorescence assay
Cytotoxicity against human K562 cells after 72 hrs by calcein AM staining-based fluorescence assay
|
[PMID: 25835357] |
| K562 | IC50 |
62 μM
Compound: 31b, (CAN508)
|
Antiproliferative activity against K562 cell line
Antiproliferative activity against K562 cell line
|
[PMID: 17064068] |
| KM12 | GI50 |
17.1 μM
Compound: CAN508
|
Cytotoxicity against human KM12 cells
Cytotoxicity against human KM12 cells
|
[PMID: 21777997] |
| LOX IMVI | GI50 |
4.1 μM
Compound: CAN508
|
Cytotoxicity against human LOXIMVI cells
Cytotoxicity against human LOXIMVI cells
|
[PMID: 21777997] |
| M14 | GI50 |
15.9 μM
Compound: CAN508
|
Cytotoxicity against human M14 cells
Cytotoxicity against human M14 cells
|
[PMID: 21777997] |
| Malme-3M | GI50 |
24.5 μM
Compound: CAN508
|
Cytotoxicity against human MALME-3M cells
Cytotoxicity against human MALME-3M cells
|
[PMID: 21777997] |
| MCF7 | GI50 |
23.5 μM
Compound: CAN508
|
Cytotoxicity against human MCF7 cells
Cytotoxicity against human MCF7 cells
|
[PMID: 21777997] |
| MCF7 | IC50 |
15 μM
Compound: CAN508
|
Inhibition of RNA synthesis in human MCF7 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting
Inhibition of RNA synthesis in human MCF7 cells assessed as decrease in [3H] Uridine incorporation after 2 hrs by scintillation counting
|
[PMID: 21777997] |
| MCF7 | IC50 |
33 μM
Compound: 31b, (CAN508)
|
Antiproliferative activity against MCF7 cell line
Antiproliferative activity against MCF7 cell line
|
[PMID: 17064068] |
| MCF7 | IC50 |
62 μM
Compound: IIIa, CAN508
|
Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM staining-based fluorescence assay
Cytotoxicity against human MCF7 cells after 72 hrs by calcein AM staining-based fluorescence assay
|
[PMID: 25835357] |
| MDA-MB-231 | GI50 |
16.7 μM
Compound: CAN508
|
Cytotoxicity against human MDA-MB-231 cells
Cytotoxicity against human MDA-MB-231 cells
|
[PMID: 21777997] |
| MDA-MB-435 | GI50 |
17.1 μM
Compound: CAN508
|
Cytotoxicity against human MDA-MB-435 cells
Cytotoxicity against human MDA-MB-435 cells
|
[PMID: 21777997] |
| MOLT-4 | GI50 |
13.5 μM
Compound: CAN508
|
Cytotoxicity against human MOLT4 cells
Cytotoxicity against human MOLT4 cells
|
[PMID: 21777997] |
| NCI/ADR-RES | GI50 |
22.5 μM
Compound: CAN508
|
Cytotoxicity against human NCI/ADR-RES cells
Cytotoxicity against human NCI/ADR-RES cells
|
[PMID: 21777997] |
| NCI-H226 | GI50 |
17.7 μM
Compound: CAN508
|
Cytotoxicity against human NCI-H226 cells
Cytotoxicity against human NCI-H226 cells
|
[PMID: 21777997] |
| NCI-H23 | GI50 |
19.1 μM
Compound: CAN508
|
Cytotoxicity against human NCI-H23 cells
Cytotoxicity against human NCI-H23 cells
|
[PMID: 21777997] |
| NCI-H322M | GI50 |
25.1 μM
Compound: CAN508
|
Cytotoxicity against human NCI-H322M cells
Cytotoxicity against human NCI-H322M cells
|
[PMID: 21777997] |
| NCI-H460 | GI50 |
25.1 μM
Compound: CAN508
|
Cytotoxicity against human NCI-H460 cells
Cytotoxicity against human NCI-H460 cells
|
[PMID: 21777997] |
| NCI-H522 | GI50 |
24.3 μM
Compound: CAN508
|
Cytotoxicity against human NCI-H522 cells
Cytotoxicity against human NCI-H522 cells
|
[PMID: 21777997] |
| OVCAR-3 | GI50 |
22.8 μM
Compound: CAN508
|
Cytotoxicity against human OVCAR3 cells
Cytotoxicity against human OVCAR3 cells
|
[PMID: 21777997] |
| OVCAR-4 | GI50 |
19 μM
Compound: CAN508
|
Cytotoxicity against human OVCAR4 cells
Cytotoxicity against human OVCAR4 cells
|
[PMID: 21777997] |
| OVCAR-5 | GI50 |
23.5 μM
Compound: CAN508
|
Cytotoxicity against human OVCAR5 cells
Cytotoxicity against human OVCAR5 cells
|
[PMID: 21777997] |
| OVCAR-8 | GI50 |
18 μM
Compound: CAN508
|
Cytotoxicity against human OVCAR8 cells
Cytotoxicity against human OVCAR8 cells
|
[PMID: 21777997] |
| PC-3 | GI50 |
20.3 μM
Compound: CAN508
|
Cytotoxicity against human PC3 cells
Cytotoxicity against human PC3 cells
|
[PMID: 21777997] |
| RPMI-8226 | GI50 |
14.4 μM
Compound: CAN508
|
Cytotoxicity against human RPMI8226 cells
Cytotoxicity against human RPMI8226 cells
|
[PMID: 21777997] |
| RPMI-8226 | IC50 |
24.9 μM
Compound: IIIa, CAN508
|
Cytotoxicity against human RPMI8226 cells after 72 hrs by calcein AM staining-based fluorescence assay
Cytotoxicity against human RPMI8226 cells after 72 hrs by calcein AM staining-based fluorescence assay
|
[PMID: 25835357] |
| RXF 393 | GI50 |
18.4 μM
Compound: CAN508
|
Cytotoxicity against human RXF393 cells
Cytotoxicity against human RXF393 cells
|
[PMID: 21777997] |
| SF-268 | GI50 |
20.6 μM
Compound: CAN508
|
Cytotoxicity against human SF268 cells
Cytotoxicity against human SF268 cells
|
[PMID: 21777997] |
| SF-295 | GI50 |
23.3 μM
Compound: CAN508
|
Cytotoxicity against human SF295 cells
Cytotoxicity against human SF295 cells
|
[PMID: 21777997] |
| SF-539 | GI50 |
13.2 μM
Compound: CAN508
|
Cytotoxicity against human SF539 cells
Cytotoxicity against human SF539 cells
|
[PMID: 21777997] |
| Sf9 | IC50 |
0.35 μM
Compound: IIIa, CAN508
|
Inhibition of CDK9/cyclin T1 (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK9/cyclin T1 (unknown origin) expressed in baculovirus infected Sf9 cells
|
[PMID: 25835357] |
| Sf9 | IC50 |
13.5 μM
Compound: IIIa, CAN508
|
Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK4/cyclin D1 (unknown origin) expressed in baculovirus infected Sf9 cells
|
[PMID: 25835357] |
| Sf9 | IC50 |
20 μM
Compound: IIIa, CAN508
|
Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected Sf9 cells
|
[PMID: 25835357] |
| Sf9 | IC50 |
26 μM
Compound: IIIa, CAN508
|
Inhibition of CDK7/cyclin H (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK7/cyclin H (unknown origin) expressed in baculovirus infected Sf9 cells
|
[PMID: 25835357] |
| Sf9 | IC50 |
44 μM
Compound: IIIa, CAN508
|
Inhibition of CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 cells
Inhibition of CDK1/cyclin B (unknown origin) expressed in baculovirus infected Sf9 cells
|
[PMID: 25835357] |
| SK-MEL-2 | GI50 |
14.4 μM
Compound: CAN508
|
Cytotoxicity against human SK-MEL-2 cells
Cytotoxicity against human SK-MEL-2 cells
|
[PMID: 21777997] |
| SK-MEL-28 | GI50 |
22.1 μM
Compound: CAN508
|
Cytotoxicity against human SK-MEL-28 cells
Cytotoxicity against human SK-MEL-28 cells
|
[PMID: 21777997] |
| SK-MEL-5 | GI50 |
13.9 μM
Compound: CAN508
|
Cytotoxicity against human SK-MEL-5 cells
Cytotoxicity against human SK-MEL-5 cells
|
[PMID: 21777997] |
| SK-OV-3 | GI50 |
49.2 μM
Compound: CAN508
|
Cytotoxicity against human SKOV3 cells
Cytotoxicity against human SKOV3 cells
|
[PMID: 21777997] |
| SN12C | GI50 |
23.3 μM
Compound: CAN508
|
Cytotoxicity against human SN12C cells
Cytotoxicity against human SN12C cells
|
[PMID: 21777997] |
| SNB-19 | GI50 |
29.9 μM
Compound: CAN508
|
Cytotoxicity against human SNB19 cells
Cytotoxicity against human SNB19 cells
|
[PMID: 21777997] |
| SNB-75 | GI50 |
18.5 μM
Compound: CAN508
|
Cytotoxicity against human SNB75 cells
Cytotoxicity against human SNB75 cells
|
[PMID: 21777997] |
| SR | GI50 |
10.3 μM
Compound: CAN508
|
Cytotoxicity against human SR cells
Cytotoxicity against human SR cells
|
[PMID: 21777997] |
| SW-620 | GI50 |
26.3 μM
Compound: CAN508
|
Cytotoxicity against human SW620 cells
Cytotoxicity against human SW620 cells
|
[PMID: 21777997] |
| T47D | GI50 |
14.2 μM
Compound: CAN508
|
Cytotoxicity against human T47D cells
Cytotoxicity against human T47D cells
|
[PMID: 21777997] |
| TK-10 | GI50 |
25.6 μM
Compound: CAN508
|
Cytotoxicity against human TK10 cells
Cytotoxicity against human TK10 cells
|
[PMID: 21777997] |
| U-251 | GI50 |
21.2 μM
Compound: CAN508
|
Cytotoxicity against human U251 cells
Cytotoxicity against human U251 cells
|
[PMID: 21777997] |
| UACC-257 | GI50 |
24.4 μM
Compound: CAN508
|
Cytotoxicity against human UACC257 cells
Cytotoxicity against human UACC257 cells
|
[PMID: 21777997] |
| UACC-62 | GI50 |
11 μM
Compound: CAN508
|
Cytotoxicity against human UACC62 cells
Cytotoxicity against human UACC62 cells
|
[PMID: 21777997] |
| UO-31 | GI50 |
13.7 μM
Compound: CAN508
|
Cytotoxicity against human UO31 cells
Cytotoxicity against human UO31 cells
|
[PMID: 21777997] |
CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays[1].
CAN508 (20-40 μM; 72 hours) significantly reduces cell proliferation in a dose dependent manner in all three esophageal adenocarcinoma cell lines (SKGT4, OE33 and FLO-1 cells) with IC50s ranging from 34.99 to 91.09 μM[2].
CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:SKGT4, OE33 and FLO-1 cells
-
Concentration:40 μM
-
Incubation Time:72 hours
-
Result:Increased apoptosis by 2 fold in all three esophageal adenocarcinoma cells compared to untreated controls.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:4 weeks-old female nude mice (esophageal adenocarcinoma xenografts)[1]
-
Dosage:60 mg/kg
-
Administration:I.p.; daily for 10 days
-
Result:Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction.
Chemical Information
-
No. CAS 140651-18-9
-
Appearance Solid
-
Peso molecular 218.22
-
Fòrmula C9H10N6O
-
Color Light yellow to yellow
-
SMILES
OC1=CC=C(/N=N/C2=C(N)NN=C2N)C=C1
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
-
Journal Impact Factor
-
Most Recent
Solvente y solubilidad
DMSO : 250 mg/mL (1145.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (9.53 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Krystof V, et al. 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006;49(22):6500-6509. [Content Brief]
[2]. Tong Z, et al. Antitumor effects of cyclin dependent kinase 9 inhibition in esophageal adenocarcinoma. Oncotarget. 2017;8(17):28696-28710. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.5825 mL | 22.9127 mL | 45.8253 mL | 114.5633 mL |
| 5 mM | 0.9165 mL | 4.5825 mL | 9.1651 mL | 22.9127 mL | |
| 10 mM | 0.4583 mL | 2.2913 mL | 4.5825 mL | 11.4563 mL | |
| 15 mM | 0.3055 mL | 1.5275 mL | 3.0550 mL | 7.6376 mL | |
| 20 mM | 0.2291 mL | 1.1456 mL | 2.2913 mL | 5.7282 mL | |
| 25 mM | 0.1833 mL | 0.9165 mL | 1.8330 mL | 4.5825 mL | |
| 30 mM | 0.1528 mL | 0.7638 mL | 1.5275 mL | 3.8188 mL | |
| 40 mM | 0.1146 mL | 0.5728 mL | 1.1456 mL | 2.8641 mL | |
| 50 mM | 0.0917 mL | 0.4583 mL | 0.9165 mL | 2.2913 mL | |
| 60 mM | 0.0764 mL | 0.3819 mL | 0.7638 mL | 1.9094 mL | |
| 80 mM | 0.0573 mL | 0.2864 mL | 0.5728 mL | 1.4320 mL | |
| 100 mM | 0.0458 mL | 0.2291 mL | 0.4583 mL | 1.1456 mL |