Catalog No.S2742 Synonyms: CAY10572

PHA-767491 Chemical Structure

Molecular Weight(MW): 249.7

PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM in cell-free assays, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fold selectivity against PLK1 and CHK2.

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Cited by 5 Publications

1 Customer Review

  • Viability at 250 nM and CI vs. Fa for U2932 following 24 hours exposure to ABT-199, additional drugs with activity against CDK9, or the combinations. Mean of quadruplicates ± SEM.

    Leukemia, 2015, 29(8):1702-12.. PHA-767491 purchased from Selleck.

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Biological Activity

Description PHA-767491 is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM in cell-free assays, respectively.It displays ~20-fold selectivity against CDK1/2 and GSK3-β, 50-fold selectivity against MK2 and CDK5, 100-fold selectivity against PLK1 and CHK2.
Features The first inhibitor that directly affects the mechanisms controlling initiation as opposed to elongation in DNA replication.
Cdc7 [1]
(Cell-free assay)
CDK9 [1]
(Cell-free assay)
GSK-3β [1]
(Cell-free assay)
CDK2 [1]
(Cell-free assay)
CDK1 [1]
(Cell-free assay)
10 nM 34 nM 220 nM 240 nM 250 nM
In vitro

PHA-767491 displays approximately 20-fold selectivity for Cdk1, Cdk2 and GSK3-β, 50-fold selectivity for MK2 and Cdk5 and 100-fold selectivity for PLK1 and CHK2. PHA-767491 inhibits cell proliferation in a variety of human cell lines with IC50 of 0.86 μM for SF-268 to 5.87 μM for K562, and significantly induces apoptosis in a p53-independent manner in almost all cell lines in contrast with 5-FU or gemcitabine which only works in a few of cell lines. Unlike current DNA synthesis inhibitors, PHA-767491 treatment at 5 μM blocks the initiation of DNA replication but not replication fork progression, due to specific inhibition of Cdc7 kinase and Mcm2 phosphorylation at the Cdc7-dependent Ser40 site. [1] The up-regulated Mcl-1 levels in ABT-737-resistant OCI-LY1 and SU-DHL-4 cells can be significantly decreased by PHA-767491 treatment at 3 μM possibly due to the inhibition of Cdk9, leading to the restoration of the sensitivity to ABT-737. [2] The direct mitochondrial dependent pro-apoptosis effect of PHA-767491 is also observed when applied at 1 μM in quiescent chronic lymphocytic leukemia (CLL) cells through the similar mechanism with EC50 of 0.34-0.97 μM. While in proliferating CLL cells stimulated by CD154 and interleukin-4, PHA-767491 treatment at 5 μM abolishes DNA synthesis by inhibiting Cdc7 rather than triggering cell death. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human SF268 cells M2X2WnBzd2yrZnXyZZRqd25iYYPzZZk> MV23NkBp NYe3Z|UySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBxPTNiZHXmbYNq\W62IHj1cYFvKFOIMk[4JINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME2wMlg3KM7:TR?= MUKxPFQ3QThyOR?=
human HCT116 cells M17IVXBzd2yrZnXyZZRqd25iYYPzZZk> MlnwO|IhcA>? M3zYTGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIV5eHKnc4PpcocheDV|IHflcoUh[W[2ZYKgO|IhcHK|IHL5JJBzd2yrZnXyZZRqfmViYYPzZZktKEmFNUC9NE46PyEQvF2= MlLENVg1Pjl6MEm=
human HCT16 cells M1LXeXBzd2yrZnXyZZRqd25iYYPzZZk> MVm3NkBp MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHLhd4VlKGG|c3H5MEBKSzVyPUGg{txO NVPpb3gyOTlzMUW4OFU>
human SW403 cells M{HQW3Bzd2yrZnXyZZRqd25iYYPzZZk> NHzxU3E4OiCq NWnNT3IxSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|QxOyClZXzsd{Bi\nSncjC3NkBpenNiYomgcJVkcW[ncnHz[UBj[XOnZDDhd5NigSxiSVO1NF0yKM7:TR?= M1:4VFE6OTF3OES1
human A2780 cells NFLIfJhRem:uaX\ldoF1cW:wIHHzd4F6 MXS3NkBp NWCyUXF{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{BmgHC{ZYPzbY5oKHB3MzDn[Y5mKGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVEvODdizszN NIXWVJAyQDR4OUiwPS=>
human SW48 cells MVHQdo9tcW[ncnH0bY9vKGG|c3H5 Mmr6O|IhcA>? MUfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNEigZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KGy3Y3nm[ZJie2ViYnHz[YQh[XO|YYmsJGlEPTB;MT6yJO69VQ>? MXuxPVEyPTh2NR?=
human MCF7 cells NI\zbGlRem:uaX\ldoF1cW:wIHHzd4F6 NV35fYVFPzJiaB?= MoPuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHLhd4VlKGG|c3H5MEBKSzVyPUGuN{DPxE1? MnjSNVkyOTV6NEW=
human U2OS cells M1vreHBzd2yrZnXyZZRqd25iYYPzZZk> NEXPdIg4OiCq MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV{T2OgZ4VtdHNiZYjwdoV{e2mwZzDwOVMh\2WwZTDh[pRmeiB5MjDodpMh[nlicILvcIln\XKjdHn2[UBie3OjeTygTWM2OD1zLkS5JO69VQ>? NVvFc2psOTh2Nkm4NFk>
human COLO205 cells NFvPUHdRem:uaX\ldoF1cW:wIHHzd4F6 MYO3NkBp M4P1UGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQ1;MU|IxPSClZXzsd{Bi\nSncjC3NkBpenNiYomgcJVkcW[ncnHz[UBj[XOnZDDhd5NigSxiSVO1NF0yNjVizszN Mle3NVkyOTV6NEW=
human OVCAR8 cells M1\4TXBzd2yrZnXyZZRqd25iYYPzZZk> NEHRWZI4OiCq MXPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IIC1N{Bl\W[rY3nlcpQhcHWvYX6gU3ZESVJ6IHPlcIx{KGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVEvPTZizszN Ml3zNVg1Pjl6MEm=
human L363 cells MkXnVJJwdGmoZYLheIlwdiCjc4PhfS=> M33XeVczKGh? MlKwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOM{[zJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHLhd4VlKGG|c3H5MEBKSzVyPUGuOkDPxE1? NYTNTph5OTlzMUW4OFU>
human NHDF cells M2DnfnBzd2yrZnXyZZRqd25iYYPzZZk> Moj6O|IhcA>? NGHvR5lCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7ISGYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZoF{\WRiYYPzZZktKEmFNUC9NU43KM7:TR?= NVPzVIhZOTlzMUW4OFU>
human NCI-H929 cells NYn2d2V1WHKxbHnm[ZJifGmxbjDhd5NigQ>? MWK3NkBp MnXORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFkzQSClZXzsd{Bi\nSncjC3NkBpenNiYomgcJVkcW[ncnHz[UBj[XOnZDDhd5NigSxiSVO1NF0yNjhizszN M1T3[VE6OTF3OES1
human SF539 cells NVjS[|lRWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml;FO|IhcA>? M3\IdmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOg[ZhxemW|c3nu[{BxPTNiZ3Xu[UBi\nSncjC3NkBpenNiYomgdJJwdGmoZYLheIl3\SCjc4PhfUwhUUN3ME2yMlM1KM7:TR?= NFPOWHkyQDR4OUiwPS=>
human SW480 cells M2W1RXBzd2yrZnXyZZRqd25iYYPzZZk> MVO3NkBp NF6wV2ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JJA2OyCmZX\pZ4lmdnRiaIXtZY4hW1d2OECgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KHC{b3zp[oVz[XSrdnWgZZN{[XluIFnDOVA:Oi54NzFOwG0> MV2xPFQ3QThyOR?=
human NCI60 cells NGH3NI9Rem:uaX\ldoF1cW:wIHHzd4F6 NWTvR3Z3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{whUUN3ME2zMlEh|ryP NHvTbZMyQDR4OUiwPS=>
human Jurkat cells NVPUWXRGWHKxbHnm[ZJifGmxbjDhd5NigQ>? Mn64O|IhcA>? MX3BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IIC1N{Bl\W[rY3nlcpQhcHWvYX6gTpVzc2G2IHPlcIx{KGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVMvOiEQvF2= NFfxTZMyQDR4OUiwPS=>
human HCT15 cells M3vpN3Bzd2yrZnXyZZRqd25iYYPzZZk> NIPYcIQ4OiCq M{W4WWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVUh[2WubIOg[ZhxemW|c3nu[{BxPTNiZ3Xu[UBi\nSncjC3NkBpenNiYomgdJJwdGmoZYLheIl3\SCjc4PhfUwhUUN3ME2zMlgyKM7:TR?= MX6xPFQ3QThyOR?=
human OPM2 cells MWjQdo9tcW[ncnH0bY9vKGG|c3H5 M4HaXFczKGh? M2XOXGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2DNNkBk\WyuczDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDiZZNm\CCjc4PhfUwhUUN3ME20MlUh|ryP MmewNVkyOTV6NEW=
human HT-29 cells MnvzVJJwdGmoZYLheIlwdiCjc4PhfS=> NU[3[HUzPzJiaB?= NGDjVZlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjUMVI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIJie2WmIHHzd4F6NCCLQ{WwQVUh|ryP M{nveFE6OTF3OES1
human K562 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 MnT2O|IhcA>? NHK0Z3hCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JJA2OyCmZX\pZ4lmdnRiaIXtZY4hUzV4MjDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;NT64O{DPxE1? NXL1fGNLOTh2Nkm4NFk>
U937 cells MVPGeY5kfGmxbjDhd5NigQ>? NWf4SFlKUW6qaXLpeIlwdiCxZjDUUmZidHCqYTDwdo9lfWO2aX;uJIlvKFV7M{egZ4VtdHNuIFnDOVA:OTlizszN MlvqNVc1QDByNkS=
human HeLa cells MlPzSpVv[3Srb36gZZN{[Xl? MX21JO69VQ>? M3v2TFI1KGh? NWPyWY1nUW6mdXP0bY9vKG:oIHHwc5B1d3OrczDpckBpfW2jbjDI[WxiKGOnbHzzJIF{e2W|c3XkJIF{KGGycHXhdoFv[2Vib3[gVGFTWCCjdDC1JJVOKGGodHXyJFI1KGi{cx?= NUXsVHUyOTh2Nkm4NFk>
NHDF MUHGeY5kfGmxbjDhd5NigQ>? NGrMcHo2KM7:TR?= NUnEcow2OTZiaB?= MUPJcoR2[3Srb36gc4Yh[2WubDDjfYNt\SCjcoLld5QhcW5idHj5cYllcW6nIHTl[olkcWWwdDDOTGRHKGG|c3Xzd4VlKGG|IFTORUB{gW62aHXzbZMhcW5iUz3wbIF{\SCjdDC1JJVOKGGodHXyJFE3cHK|IF\BR3Mh[W6jbInzbZMhcW5icILld4Vv[2Vib3[gd4VzfW1? MXSxPFQ3QThyOR?=

... Click to View More Cell Line Experimental Data

In vivo Administration of PHA-767491 twice a day for 5 days significantly inhibits the growth of HL60 xenograft in a dose-dependent manner with TGI of 50% and 92% at dose of 20 mg/kg and 30 mg/kg, respectively, the effect of which is also marked in A2780, Mx-1, and HCT-116 xenograft models as well as the DMBA-induced mammary carcinomas, and correlates with Cdc7 inhibition and subsequently decreased phosphorylation of Mcm2 at the Cdc7-dependent site Ser40 [1]


Kinase Assay:[1]
+ Expand

In vitro kinase assays:

The inhibition of Cdc7 and Cdk9 by PHA-767491 (IC50) is determined using the strong anion exchanger (Dowex 1-X8 resin, formate form)-based assay. For each enzyme, the absolute Km values for ATP and the specific substrate are initially determined, and each assay is then run at optimized ATP/33P-γ-ATP mix (2Km) and substrate (5Km) concentrations. Cdc7 kinase assay is performed in a buffer containing 50 mM Hepes pH 7.9, 15 mM MgCl2, 2 mM β- glycerylphosphate, 0.2 mg/mL BSA, 1 mM DTT, 3 μM Na3VO4, 2Km ATP/33P-γ-ATP mix, 5Km Mcm2 (aa 10-294), 37 nM of recombinant Cdc7/Dbf4 and increasing concentration of PHA-767491 in a final volume of 30 μL, and incubated for 1 hour at 25 °C. Cdk9 kinase assay is performed using 50 nM of recombinant Cdk9/cyclin T in 50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM DTT, 3 μM Na3VO4, 2Km ATP/33P-γ-ATP mix, 5Km RNA polymerase CDT peptide and increasing concentration of PHA-767491 in a final volume of 30 μL, and incubated for 1 hour at 25 °C. After incubation, an amount of 150 μL of resin/formate (pH 3.0) is added to stop the reaction and capture unreacted 33P-γ-ATP, separating it from the phosphorylated substrate in solution. After 1 hour of rest, a volume of 50 μL supernatant is transferred to Optiplate 96-well plates. After the additon of 150 μL of Microscint 40, the radioactivity is counted in the TopCount.
Cell Research:[1]
+ Expand
  • Cell lines: HeLa, MCF7, HCT-116, U2OS, A2780, K562, SF-539, SF-268, Ovcar8, SW480, COLO205, HCT-15, Jurkat, PC3, and NHDF
  • Concentrations: Dissolved in DMSO, final concentrations ~ 20 μM
  • Incubation Time: 24 or 72 hours
  • Method: Cells are exposed to PHA-767491 for 24 or 72 hours. Cells are lysed and the ATP content in the well, used as a measure of viable cells, is determined using a thermostable firefly luciferase–based assay. Activation of caspase-3 and caspase-7 is measured as a ratio between treated sample and untreated control with a luciferase-based assay, containing a specific proluminescent substrate. DNA replication is measured as incorporation of nucleotide analog BrdU into DNA by flow cytometry.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Female SCID mice subcutaneously implanted with HL60 cells, male Hsd, athymic nu-nu mice subcutaneously implanted with HCT116 cells, A2780 or Mx-1 cells, and female Sprague-Dawley rats with DMBA-induced mammary carcinomas
  • Formulation: Dissolved in DMSO, and diluted in saline
  • Dosages: ~50 mg/kg
  • Administration: Intravenous or oral administration twice a day
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 24 mg/mL (96.11 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

* 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 249.7


CAS No. 942425-68-5
Storage powder
in solvent
Synonyms CAY10572

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID