JNJ-7706621
Based on 4 publication(s) in Google Scholar
JNJ-7706621 is a potent aurora kinase inhibitor, and also inhibits CDK1 and CDK2, with IC50s of 9 nM, 3 nM, 11 nM, and 15 nM for CDK1, CDK2, aurora-A and aurora-B, respectively.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.39%
- CAS No.: 443797-96-4
- 화학식: C15H12F2N6O3S
- 분자량:394.36
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) JNJ-7706621
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Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
All Aurora Kinase Isoforms
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Biological Activity
제품 설명
IC50 & Target
[3]|
CDK6/cyclinD1 175 nM (IC50) |
CDK2/cyclinE 3 nM (IC50) |
Cdk4/cyclin D1 253 nM (IC50) |
Cdk1/cyclin B 9 nM (IC50) |
cdk2/cyclin A 4 nM (IC50) |
CDK3/Cyclin E 58 nM (IC50) |
Aurora A 11 nM (IC50) |
Aurora B 15 nM (IC50) |
VEGF-R2 154 nM (IC50) |
VEGF-R1 6400 nM (IC50) |
VEGF-R3 735 nM (IC50) |
FGF-R1 575 nM (IC50) |
FGF-R2 226 nM (IC50) |
GSK3β 254 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
0.45 μM
Compound: 3b
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In vitro inhibitory concentration against cell proliferation in human A375 (malignant melanoma),tumor cells
In vitro inhibitory concentration against cell proliferation in human A375 (malignant melanoma),tumor cells
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[PMID: 15974571] |
| A-375 | IC50 |
447 nM
Compound: JNJ-7706621
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Antiproliferative activity against human A375 cells
Antiproliferative activity against human A375 cells
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[PMID: 16682186] |
| HCT-116 | IC50 |
0.25 μM
Compound: 3b
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In vitro inhibitory concentration against cell proliferation in human HCT116 (colon carcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in human HCT116 (colon carcinoma) tumor cells
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[PMID: 15974571] |
| HCT-116 | IC50 |
254 nM
Compound: JNJ-7706621
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Antiproliferative activity against human HCT116 cells
Antiproliferative activity against human HCT116 cells
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[PMID: 16682186] |
| HeLa | IC50 |
0.28 μM
Compound: 3b
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In vitro inhibitory concentration against cell proliferation in human HeLa (cervical adenocarcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in human HeLa (cervical adenocarcinoma) tumor cells
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[PMID: 15974571] |
| HeLa | IC50 |
284 nM
Compound: JNJ-7706621
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Antiproliferative activity against human HeLa cells
Antiproliferative activity against human HeLa cells
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[PMID: 16682186] |
| MDA-MB-231 | IC50 |
0.59 μM
Compound: 3b
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In vitro inhibitory concentration against cell proliferation in various human MDA-MB-231 (breast carcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in various human MDA-MB-231 (breast carcinoma) tumor cells
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[PMID: 15974571] |
| PC-3 | IC50 |
0.12 μM
Compound: 3b
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In vitro inhibitory concentration against cell proliferation in human PC-3 (prostate adenocarcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in human PC-3 (prostate adenocarcinoma) tumor cells
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[PMID: 15974571] |
| SK-OV-3 | IC50 |
0.75 μM
Compound: 3b
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In vitro inhibitory concentration against cell proliferation in human SK-OV-3 (ovarian adenocarcinoma) tumor cells
In vitro inhibitory concentration against cell proliferation in human SK-OV-3 (ovarian adenocarcinoma) tumor cells
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[PMID: 15974571] |
In Vitro
JNJ-7706621 shows antiproliferative activity against various human tumor cells with IC50s of 284, 254, and 447 nM for HeLa, HCT116, and A375, respectively[1]. JNJ-7706621 inhibits other centrosomal proteins such as TOG, Nek2, and TACC3 in early mitotic phase, but does not prevent localization of Aurora A to the spindle poles. Treatment of nocodazole-synchronized cells with JNJ-7706621 can override mitotic arrest by preventing spindle checkpoint signaling, resulting in failure of chromosome alignment and segregation[2]. JNJ-7706621 shows inhibition of Aurora-A and Aurora-B but has no activity at the highest concentration tested on the Plk1 or Wee1 serine/threonine kinases. JNJ-7706621 also shows potent growth inhibition in vitro on all human cancer cell types with IC50 values ranging from 112 to 514 nM[3]. JNJ-7706621 suspensions inhibits cell viability of HeLa cells with IC50s of 2.1 and 0.9 μg/mL at 24 and 48 h. The IC50 of the JNJ-7706621-loaded nanoparticles are 35 and 2.7 μg/mL and the IC50 of the JNJ-7706621-loaded micelles are 6.3 and 1.6 μg/mL[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 443797-96-4
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Appearance Solid
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분자량 394.36
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화학식 C15H12F2N6O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(NC2=NN(C(C3=C(F)C=CC=C3F)=O)C(N)=N2)C=C1)(N)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Chem Biol
2019 Sep 19;26(9):1263-1273.e5. PMID: 31257183
JNJ-7706621 purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2019 Sep 19;26(9):1263-1273.e5. [Abstract]
JNJ-7706621 (compound 1; 0.1, 1, 10, 100 μM) concentration-dependent inhibition of the steady-state ATPase activity of spastin wild-type (WT) and three constructs with mutations at variability hot-spot residues (Q488V, N527C and T692A). (Drosophila melanogaster spastin, aa 209–758, hereafter spastin-WT, IC50: 5.8 ± 0.6 µM, 0.5 mM MgATP).
JNJ-7706621 purchased from MedChemExpress. Usage Cited in: Cell Chem Biol. 2019 Sep 19;26(9):1263-1273.e5. [Abstract]
JNJ-7706621 (compound 1; 1.25, 2.5, 5, 10, 20, 40 μM) concentration-dependent inhibition of the steady-state ATPase activity of spastin wild-type (WT).
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EMBO Mol Med
Isomeranzin activates Gnas-AMPK signaling to drive white adipose browning and curb obesity in mice. [Abstract]2025 Nov 26. PMID: 41299101 -
J Invest Dermatol
Pharmacological Characterization of Zasocitinib (TAK-279): An Oral, Highly Selective, and Potent Allosteric TYK2 Inhibitor. [Abstract]2025 May 27:S0022-202X(25)00531-7. PMID: 40441292 -
BMC Cancer
Artificial intelligence to guide precision anticancer therapy with multitargeted kinase inhibitors. [Abstract]2022 Nov 24;22(1):1211. PMID: 36434556
JNJ-7706621 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2022 Nov 24;22(1):1211. [Abstract]
JNJ-7706621 (1, 3.162, 10, 31.62, 100, 316.2 nM; 1, 3.162, 10 μM; 3 days) inhibited Panc 04.03 cell viability.
JNJ-7706621 purchased from MedChemExpress. Usage Cited in: BMC Cancer. 2022 Nov 24;22(1):1211. [Abstract]
JNJ-7706621 (10 μM; 3 days) inhibited Panc 04.03 cell viability.
용액&용해도
In Vitro:
DMSO : ≥ 125 mg/mL (316.97 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. 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)
In Vivo:
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 (5.27 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
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.
Protocol
Kinase Assay[4]
To identify compounds that inhibit CDK1 kinase activity, a screening method is developed using the CDK1/cyclin B complex to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylatedin vivo by CDK1. Inhibition of CDK1 activity is measured by observing a reduced amount of 33P-g-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 AM peptide, 0.1 ACi per well 33P-g-ATP (2,000-3,000 Ci/mmol), and 5 AM ATP in the presence or absence of various concentrations of test compound and incubated at 30°C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. Linear regression analysis of the percent inhibition by test compound is used to determine IC50 values. The Aurora kinase assays are done with 10 AM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay[3]
HeLa cells are seeded in 96-well plates at the density of 2500 viable cells per well. The cells are then incubated with a suspension of JNJ-7706621, JNJ-7706621-loaded micelles and nanoparticles (JNJ-7706621 concentrations of 0.011, 0.022, 0.11, 0.22, 1.1, 2.2, 11 and 22 μg/mL; dilutions are made in the medium) and drug-free polymeric micelles (polymers concentrations 0.3 mg/mL) and nanoparticles (polymers concentration 5 mg/mL) for 4, 24 and 48 h. The cytotoxicity is assessed using the MTT test. Absorbance is measured at 570 nm using a microplate reader. Untreated cells are taken as control with 100% viability and Triton X-100 1% is used as positive control of cytotoxicity. The results are expressed as mean values ± standard deviations of five measurements.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[4]
Briefly, animals are implanted s.c. with 1 mm3 A375 tumor fragments in the hindflank. After tumors reach 62 to 126 mg, groups are pair matched. Animals are given JNJ-7706621 or vehicle control starting on day 1. The tumor growth delay method is followed where each animal is euthanized when its neoplasm reached a predetermined size of 2.0 g. All statistical analyses are conducted using unpaired t tests at a P level of 0.05 (two tailed).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (286 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Huang S, et al. Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. Epub 2006 May 6. [Content Brief]
[2]. Matsuhashi A, et al. Growth suppression and mitotic defect induced by JNJ-7706621, an inhibitor of cyclin-dependent kinases and aurora kinases. Curr Cancer Drug Targets. 2012 Jul;12(6):625-39. [Content Brief]
[3]. Emanuel S, et al. The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Cancer Res. 2005 Oct 1;65(19):9038-46. [Content Brief]
[4]. Danhier F, et al. Active and passive tumor targeting of a novel poorly soluble cyclin dependent kinase inhibitor, JNJ-7706621. Int J Pharm. 2010 Jun 15;392(1-2):20-8. [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. 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 | 2.5358 mL | 12.6788 mL | 25.3575 mL | 63.3939 mL |
| 5 mM | 0.5072 mL | 2.5358 mL | 5.0715 mL | 12.6788 mL | |
| 10 mM | 0.2536 mL | 1.2679 mL | 2.5358 mL | 6.3394 mL | |
| 15 mM | 0.1691 mL | 0.8453 mL | 1.6905 mL | 4.2263 mL | |
| 20 mM | 0.1268 mL | 0.6339 mL | 1.2679 mL | 3.1697 mL | |
| 25 mM | 0.1014 mL | 0.5072 mL | 1.0143 mL | 2.5358 mL | |
| 30 mM | 0.0845 mL | 0.4226 mL | 0.8453 mL | 2.1131 mL | |
| 40 mM | 0.0634 mL | 0.3170 mL | 0.6339 mL | 1.5848 mL | |
| 50 mM | 0.0507 mL | 0.2536 mL | 0.5072 mL | 1.2679 mL | |
| 60 mM | 0.0423 mL | 0.2113 mL | 0.4226 mL | 1.0566 mL | |
| 80 mM | 0.0317 mL | 0.1585 mL | 0.3170 mL | 0.7924 mL | |
| 100 mM | 0.0254 mL | 0.1268 mL | 0.2536 mL | 0.6339 mL |
JNJ-7706621 Related Classifications
HY-10329 Related Classifications
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