For research use only.

Catalog No.S2742 Synonyms: CAY10572

22 publications

PHA-767491 Chemical Structure

CAS No. 942425-68-5

PHA-767491 (CAY10572) 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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Selleck's PHA-767491 has been cited by 22 publications

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Biological Activity

Description PHA-767491 (CAY10572) 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 MUDQdo9tcW[ncnH0bY9vKGG|c3H5 MY[3NkBp NIDXeIdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JJA2OyCmZX\pZ4lmdnRiaIXtZY4hW0Z{NkigZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUCuPFYh|ryP NH3iS20yQDR4OUiwPS=>
human HCT116 cells MkLlVJJwdGmoZYLheIlwdiCjc4PhfS=> MYm3NkBp MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDlfJBz\XO|aX7nJJA2OyCpZX7lJIFnfGW{IEeyJIhzeyCkeTDwdo9tcW[ncnH0bZZmKGG|c3H5MEBKSzVyPUCuPVch|ryP MonJNVg1Pjl6MEm=
human HCT16 cells M1;tVXBzd2yrZnXyZZRqd25iYYPzZZk> NFP0[Yg4OiCq M2LYVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVYh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZoF{\WRiYYPzZZktKEmFNUC9NUDPxE1? NIfRSnEyQTFzNUi0OS=>
human SW403 cells NVjTTJhnWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml7XO|IhcA>? M1rSPWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2e0NFMh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZoF{\WRiYYPzZZktKEmFNUC9NUDPxE1? NIjjV4cyQTFzNUi0OS=>
human A2780 cells MlKyVJJwdGmoZYLheIlwdiCjc4PhfS=> MlnPO|IhcA>? NE\jT25CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyO|gxKGOnbHzzJIV5eHKnc4PpcocheDV|IHflcoUh[W[2ZYKgO|IhcHK|IHL5JJBzd2yrZnXyZZRqfmViYYPzZZktKEmFNUC9NU4xPyEQvF2= MU[xPFQ3QThyOR?=
human SW48 cells M{nPfnBzd2yrZnXyZZRqd25iYYPzZZk> NHn4dIc4OiCq NFXCbllCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOFgh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZoF{\WRiYYPzZZktKEmFNUC9NU4zKM7:TR?= M{LQd|E6OTF3OES1
human MCF7 cells Mny3VJJwdGmoZYLheIlwdiCjc4PhfS=> NWPV[IhoPzJiaB?= M3TMV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDiZZNm\CCjc4PhfUwhUUN3ME2xMlMh|ryP MUixPVEyPTh2NR?=
human U2OS cells MXHQdo9tcW[ncnH0bY9vKGG|c3H5 NFjWSVc4OiCq MlXrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCXMl;TJINmdGy|IHX4dJJme3OrbnegdFU{KGenbnWgZYZ1\XJiN{KgbJJ{KGK7IIDyc4xq\mW{YYTpeoUh[XO|YYmsJGlEPTB;MT60PUDPxE1? MX[xPFQ3QThyOR?=
human COLO205 cells MULQdo9tcW[ncnH0bY9vKGG|c3H5 NULWUnJxPzJiaB?= MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEORTF:yNFUh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZoF{\WRiYYPzZZktKEmFNUC9NU42KM7:TR?= M3XpNVE6OTF3OES1
human OVCAR8 cells M4DMfHBzd2yrZnXyZZRqd25iYYPzZZk> MWO3NkBp MV7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IIC1N{Bl\W[rY3nlcpQhcHWvYX6gU3ZESVJ6IHPlcIx{KGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVEvPTZizszN M3fJUVE5PDZ7OEC5
human L363 cells NXna[JU3WHKxbHnm[ZJifGmxbjDhd5NigQ>? NUmxb3poPzJiaB?= NX;Qc5ZVSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMN|Y{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIJie2WmIHHzd4F6NCCLQ{WwQVEvPiEQvF2= NFW3OWQyQTFzNUi0OS=>
human NHDF cells NWGwXVl2WHKxbHnm[ZJifGmxbjDhd5NigQ>? NYHHT2g4PzJiaB?= MnW2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQSFTGJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHLhd4VlKGG|c3H5MEBKSzVyPUGuOkDPxE1? Ml3JNVkyOTV6NEW=
human NCI-H929 cells MmD2VJJwdGmoZYLheIlwdiCjc4PhfS=> MUC3NkBp MWfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IPVI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIJie2WmIHHzd4F6NCCLQ{WwQVEvQCEQvF2= MmLBNVkyOTV6NEW=
human SF539 cells NUTNVFRkWHKxbHnm[ZJifGmxbjDhd5NigQ>? MknGO|IhcA>? NWHPcWZOSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTSlU{QSClZXzsd{BmgHC{ZYPzbY5oKHB3MzDn[Y5mKGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVIvOzRizszN NUHjW4NqOTh2Nkm4NFk>
human SW480 cells NYK2O4FWWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1H1U|czKGh? Mn;QRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDwOVMh\GWoaXPp[Y51KGi3bXHuJHNYPDhyIHPlcIx{KGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVIvPjdizszN Moj0NVg1Pjl6MEm=
human NCI60 cells NXjpfXdEWHKxbHnm[ZJifGmxbjDhd5NigQ>? NYXZOVgySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{whUUN3ME2zMlEh|ryP MmnCNVg1Pjl6MEm=
human Jurkat cells Mn\qVJJwdGmoZYLheIlwdiCjc4PhfS=> MX[3NkBp NHHFSplCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JJA2OyCmZX\pZ4lmdnRiaIXtZY4hUnW{a3H0JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCycn;sbYZmemG2aY\lJIF{e2G7LDDJR|UxRTNwMjFOwG0> M4KzRlE5PDZ7OEC5
human HCT15 cells NHf0ZVVRem:uaX\ldoF1cW:wIHHzd4F6 MWW3NkBp MVrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG1JINmdGy|IHX4dJJme3OrbnegdFU{KGenbnWgZYZ1\XJiN{KgbJJ{KGK7IIDyc4xq\mW{YYTpeoUh[XO|YYmsJGlEPTB;Mz64NUDPxE1? Ml[5NVg1Pjl6MEm=
human OPM2 cells Mme0VJJwdGmoZYLheIlwdiCjc4PhfS=> MknVO|IhcA>? M1jjVGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iT2DNNkBk\WyuczDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDiZZNm\CCjc4PhfUwhUUN3ME20MlUh|ryP MUGxPVEyPTh2NR?=
human HT-29 cells M3[3dnBzd2yrZnXyZZRqd25iYYPzZZk> NELodlk4OiCq MWDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHLhd4VlKGG|c3H5MEBKSzVyPUWg{txO NIjz[HkyQTFzNUi0OS=>
human K562 cells MlT5VJJwdGmoZYLheIlwdiCjc4PhfS=> M4W2WVczKGh? MonyRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDwOVMh\GWoaXPp[Y51KGi3bXHuJGs2PjJiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTVwOEeg{txO NEXTS2cyQDR4OUiwPS=>
U937 cells NXXwS|VqTnWwY4Tpc44h[XO|YYm= MofWTY5pcWKrdHnvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIHnuJHU6OzdiY3XscJMtKEmFNUC9NVkh|ryP MVixO|Q5ODB4NB?=
human HeLa cells MnqzSpVv[3Srb36gZZN{[Xl? MYq1JO69VQ>? MkfjNlQhcA>? MXLJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEinTHGgZ4VtdHNiYYPz[ZN{\WRiYYOgZZBx\WG{YX7j[UBw\iCSQWLQJIF1KDVidV2gZYZ1\XJiMkSgbJJ{ MWWxPFQ3QThyOR?=
NHDF M{exXWZ2dmO2aX;uJIF{e2G7 NU[0[YR7PSEQvF2= NFi4U3IyPiCq NWrMSo92UW6mdXP0bY9vKG:oIHPlcIwh[3mlbHWgZZJz\XO2IHnuJJRpgW2rZHnu[UBl\W[rY3nlcpQhVkiGRjDhd5Nme3OnZDDhd{BFVkFic4nueIhme2m|IHnuJHMueGijc3WgZZQhPSC3TTDh[pRmeiBzNnjyd{BHSUOVIHHuZYx6e2m|IHnuJJBz\XOnbnPlJI9nKHOncoXt M4nC[|E5PDZ7OEC5

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-MCM2 / CDC7 ; 

PubMed: 24902048     

HeLa cells were treated with PHA-767491 for the indicated time. Protein extracts were prepared and analysed by western blot with the indicated antibodies.

RNA Pol II / p-RNA Pol II / Caspase-3 / PARP / Mcl-1 / XIAP / Bcl-xL / Bcl-2 / NOXA; 

PubMed: 24202326     

KMS-18 and MM1S myeloma cells were incubated with 5 μM PHA-767491 for the indicated time. Protein extracts were prepared and analyzed by immunoblotting using the indicated antibodies

24902048 24202326
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]
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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]
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  • 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]
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  • 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
  • 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
Smiles C1CNC(=O)C2=C1NC(=C2)C3=CC=NC=C3.Cl

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID