JNJ-7706621

Catalog No.S1249

For research use only.

JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.

JNJ-7706621 Chemical Structure

CAS No. 443797-96-4

Selleck's JNJ-7706621 has been cited by 21 publications

Purity & Quality Control

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Biological Activity

Description JNJ-7706621 is pan-CDK inhibitor with the highest potency on CDK1/2 with IC50 of 9 nM/4 nM and showing >6-fold selectivity for CDK1/2 than CDK3/4/6 in cell-free assays. It also potently inhibits Aurora A/B and has no activity on Plk1 and Wee1.
Features A broad-spectrum inhibitor.
Targets
CDK2/CyclinE [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
Aurora A [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
Click to View More Targets
3 nM 4 nM 9 nM 11 nM 15 nM
In vitro

JNJ-7706621 also shows some inhibition to VEGF-R2, FGF-R2, and GSK3β, with IC50 of 154-254 nM. JNJ-7706621 shows inhibitory effect on a panel of human cancer cell types, including HeLa, HCT-116, SK-OV-3, PC3, DU145, A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with IC50 of 112-514 nM, independent of p53, retinoblastoma, or P-glycoprotein status. JNJ-7706621 is several-fold less potent at inhibiting growth of normal cell types, including MRC-5, HASMC, HUVEC, and HMVEC, with IC50 of 3.67-5.42 μM. In HeLa or U937 cells, JNJ-7706621 (0.5-3 μM) delays exit from G1, arrests cells in G2-M, induces endoreduplication, activates apoptosis, and reduces colony formation. [1] In a HeLa cell line, incremental treatment with increasing concentrations of JNJ-7706621 leads to a 16-fold resistance, which may be mediated by ABCG2. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PC3 cells MonUSpVv[3Srb36gZZN{[Xl? NYHqTm1nUW5idnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGi3bXHuJHBENTNiKIDyc5N1[XSnIHHk[Y5w[2G{Y3nuc41iMSC2dX3vdkBk\WyuczygTWM2OD1yLkGyJO69VQ>? NUnnenl2OTV7N{S1O|E>
HCT116 cells M4nwemZ2dmO2aX;uJIF{e2G7 NUXxVVBVUW5idnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGi3bXHuJGhEXDFzNjCoZ49td25iY3HyZ4lvd22jKTD0eY1weiClZXzsd{whUUN3ME2wMlI2KM7:TR?= M2fnXFE2QTd2NUex
human HeLa cells MWjGeY5kfGmxbjDhd5NigQ>? NY\XOoRFUW5idnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGi3bXHuJGhmVGFiKHPldpZq[2GuIHHk[Y5w[2G{Y3nuc41iMSC2dX3vdkBk\WyuczygTWM2OD1yLkK4JO69VQ>? NELvVIgyPTl5NEW3NS=>
human A375 cells MoTYVJJwdGmoZYLheIlwdiCjc4PhfS=> NEfCSnBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGzO|Uh[2WubIOsJGlEPTB;MD60OFch|ryP MXKxOlY5OjF6Nh?=
MDA-MB-231 cells NFXud3ZHfW6ldHnvckBie3OjeR?= NXK2R25PUW5idnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgZ4VtdCCycn;sbYZmemG2aX;uJIlvKH[jcnnveZMhcHWvYX6gUWRCNU2ELUKzNUAp[nKnYYP0JINiemOrbn;tZUkhfHWvb4KgZ4VtdHNuIFnDOVA:OC53OTFOwG0> MVixOVk4PDV5MR?=
SK-OV-3 cells MYfGeY5kfGmxbjDhd5NigQ>? NYi5SWJRUW5idnn0do8hcW6qaXLpeI9zgSClb37j[Y51emG2aX;uJIFo[Wmwc4SgZ4VtdCCycn;sbYZmemG2aX;uJIlvKGi3bXHuJHNMNU:YLUOgLI93[XKrYX6gZYRmdm:lYYLjbY5wdWFrIIT1cY9zKGOnbHzzMEBKSzVyPUCuO|Uh|ryP MknQNVU6PzR3N{G=
In vivo In mouse xenograft model of A375 melanoma human tumor, JNJ-7706621 (100 or 125 mg/kg) causes tumor regression. [3]

Protocol (from reference)

Kinase Assay:[1]
  • In vitro kinase assay for CDK1 and Aurora kinases:

    For CDK1 kinase activity, a method is developed using the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a reduced amount of 33P-γ-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 Na3VO 4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 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 JNJ-7706621 is used to determine IC50. The Aurora kinase assays are done with 10 μM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif.

Cell Research:[3]
  • Cell lines: HeLa, HCT-116, A375, SK-OV-3, MDA-MB-231, and PC-3 cells
  • Concentrations: 1 nM - 10 μM, dissolved in DMSO
  • Incubation Time: 48 hours
  • Method: The ability of JNJ-7706621 to inhibit the proliferation of cell growth is determined by measuring incorporation of 14C-labelled thymidine into newly synthesized DNA within the cells. Cells are trypsinized and counted and 3-8 × 103 cells are added to each well of a 96-well CytoStar tissue culture treated scintillating microplate in complete medium in a volume of 100 μL. Cells are incubated for 24 hours in complete medium at 37 °C in an atmosphere containing 5% CO2. Next, 1 μL of JNJ-7706621 is added to the wells of the plate. Cells are incubated for 24 more hours. Methyl 14C-thymidine 56 mCi/mmol is diluted in complete medium and 0.2 μCi/well is added to each well of the CytoStar plate in a volume of 20 μL. The plate is incubated for 24 hours at 37 °C in JNJ-7706621 plus 14C-thymidine. The contents of the plate are discarded and the plate is washed twice with 200 μL PBS. 200 μL of PBS is added to each well. The top of the plate is sealed with a transparent plate sealer and a white plate backing sealer is applied to the bottom of the plate. The degree of methyl 14C-thymidine incorporation is quantified on a Packard Top Count.
Animal Research:[1]
  • Animal Models: Mouse xenograft model of A375 cells
  • Dosages: 100 or 125 mg/kg
  • Administration: Orally or by intraperitoneal injection injection

Solubility (25°C)

In vitro

DMSO 79 mg/mL
(200.32 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% methylcellulose+0.2% Tween 80
For best results, use promptly after mixing.

14 mg/mL

Chemical Information

Molecular Weight 394.36
Formula

C15H12F2N6O3S

CAS No. 443797-96-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=C(C(=C1)F)C(=O)N2C(=NC(=N2)NC3=CC=C(C=C3)S(=O)(=O)N)N)F

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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