JNJ-7706621

Catalog No.S1249

JNJ-7706621 Chemical Structure

Molecular Weight(MW): 394.36

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.

Size Price Stock Quantity  
In DMSO USD 235 In stock
USD 120 In stock
USD 210 In stock
USD 370 In stock
USD 870 In stock
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5 Customer Reviews

  • JNJ-7706621 treatment of tamoxifen-resistant cell lines leads to arrest in the G2 cell cycle phase. M phase cells from the upper right quadrants were quantified relative to total G2/M phase cells. Statistical significant differences from vehicle-treated cells are denoted by asterisks; *P<0.05, **P<0.01.

    Oncogene 2014 10.1038/onc.2014.351. JNJ-7706621 purchased from Selleck.

    J558 cells were treated with RO3306 (5-15 umol/L), or JNJ7706621 (0.2-4 umol/L) for 6 hours, after which Western blot analysis was performed to monitor XBP-1s expression.

    Mol Cancer Ther 2014 13(3), 662-74. JNJ-7706621 purchased from Selleck.

  • C) CDK1 activity is inhibited by phosphorylation of Thr14/Tyr15 residues. Dephosphorylation of these residues activates CDK1 and promotes GVBD. In Flavopiridol-treated oocytes, the level of pCDK1 did not change compared with the control group, but Dinaciclib, and less potently JNJ, elevated the level of inhibitory phosphorylation of CDK1. In all groups, the level of pCDK1 was normalized with pan CDK1.

    PLoS One, 2016, 11(3):e0152254. JNJ-7706621 purchased from Selleck.

    Western blot analysis of p-histone , histone, Aurora A and p-Aurora A/B/C. 0-10μM JNJ-7706621 was added.

     

     

    Dr. Zhang of Tianjin Medical University. JNJ-7706621 purchased from Selleck.

  • For MTT assays, cells (2,000 ~ 5,000 cells/well) were subcultured into 96-well plates according to their growth properties. Cell proliferation was assayed at 72 hr after treatment of JNJ-7706621 by adding 20 μl of 5 mg/ml 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution per 100 μl of growth medium. After incubating for 3-4 h at 37°C, the media were removed and 150 µl/well of MTT solvent (either absolute DMSO or isopropanol containing 4 μM HCl and 0.1% Nonidet-40) was added to dissolve the formazan. The absorbance of each well was measured by ELx808 (BioTek, Winooski, VT) or Wallac Victor2 (Perkin-Elmer Life Sciences, Boston, MA) Microplate Reader. Viable cells are presented as percent of control, vehicle-treated cells.

    Dr. Yong-Weon Yi from Georgetown University Medical Center. JNJ-7706621 purchased from Selleck.

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)
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 NVvuSmR{TnWwY4Tpc44h[XO|YYm= NFXWb49KdiC4aYTyc{BqdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDj[YxtKHC{b3zp[oVz[XSrb36gbY4hcHWvYX6gVGMuOyBqcILvd5RifGViYXTlco9k[XKlaX7vcYEqKHS3bX;yJINmdGy|LDDJR|UxRTBwMUKg{txO M{jHZ|E2QTd2NUex
HCT116 cells Mlu3SpVv[3Srb36gZZN{[Xl? MlT0TY4hfmm2cn:gbY5pcWKrdH;yfUBkd26lZX70doF1cW:wIHHnZYlve3RiY3XscEBxem:uaX\ldoF1cW:wIHnuJIh2dWGwIFjDWFEyPiBqY3;sc44h[2G{Y3nuc41iMSC2dX3vdkBk\WyuczygTWM2OD1yLkK1JO69VQ>? MVGxOVk4PDV5MR?=
human HeLa cells NHXFdY1HfW6ldHnvckBie3OjeR?= NG\4fGpKdiC4aYTyc{BqdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDj[YxtKHC{b3zp[oVz[XSrb36gbY4hcHWvYX6gTIVN[SBqY3Xyeolk[WxiYXTlco9k[XKlaX7vcYEqKHS3bX;yJINmdGy|LDDJR|UxRTBwMkig{txO M17JWlE2QTd2NUex
human A375 cells NVPmWZRiWHKxbHnm[ZJifGmxbjDhd5NigQ>? MUjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNuIFnDOVA:OC52NEeg{txO M3rvVVE3Pjh{MUi2
MDA-MB-231 cells NVjmXXc1TnWwY4Tpc44h[XO|YYm= M3rDUGlvKH[rdILvJIlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IHPlcIwheHKxbHnm[ZJifGmxbjDpckB3[XKrb4XzJIh2dWGwIF3ERU1OSi1{M{GgLIJz\WG|dDDjZZJkcW6xbXGpJJR2dW:{IHPlcIx{NCCLQ{WwQVAvPTlizszN NV\4[XRrOTV7N{S1O|E>
SK-OV-3 cells NFXJWoZHfW6ldHnvckBie3OjeR?= NEnLendKdiC4aYTyc{BqdmirYnn0c5J6KGOxbnPlcpRz[XSrb36gZYdicW6|dDDj[YxtKHC{b3zp[oVz[XSrb36gbY4hcHWvYX6gV2suV1ZvMzCoc5ZiemmjbjDh[IVvd2OjcnPpco9u[SlidIXtc5Ih[2WubIOsJGlEPTB;MD63OUDPxE1? MkHHNVU6PzR3N{G=

... Click to View More Cell Line Experimental Data

In vivo In mouse xenograft model of A375 melanoma human tumor, JNJ-7706621 (100 or 125 mg/kg) causes tumor regression. [3]

Protocol

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Mouse xenograft model of A375 cells
  • Formulation: Dissolved in 0.5% methylcellulose containing 0.1% polysorbate 80 in sterile water.
  • Dosages: 100 or 125 mg/kg
  • Administration: Orally or by intraperitoneal injection injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 79 mg/mL (200.32 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
0.5% methylcellulose+0.2% Tween 80
14 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 394.36
Formula

C15H12F2N6O3S

CAS No. 443797-96-4
Storage powder
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID