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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In DMSO USD 120 In stock
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Cited by 15 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 NF;Cc4RRem:uaX\ldoF1cW:wIHHzd4F6 MmDiO|IhcA>? M1vrfmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgdFU{KGSnZnnjbYVvfCCqdX3hckBUTjJ4ODDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;MD64OkDPxE1? Ml7ZNVg1Pjl6MEm=
human HCT116 cells MXPQdo9tcW[ncnH0bY9vKGG|c3H5 MXu3NkBp NH[4UJZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{BmgHC{ZYPzbY5oKHB3MzDn[Y5mKGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVAvQTdizszN NFvlUXAyQDR4OUiwPS=>
human HCT16 cells NXTSPVJCWHKxbHnm[ZJifGmxbjDhd5NigQ>? M1OycFczKGh? NHfn[5ZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFE3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIJie2WmIHHzd4F6NCCLQ{WwQVEh|ryP M2Pq[lE6OTF3OES1
human SW403 cells M1r4R3Bzd2yrZnXyZZRqd25iYYPzZZk> NHy5Z3g4OiCq MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNECzJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHLhd4VlKGG|c3H5MEBKSzVyPUGg{txO M3TEOFE6OTF3OES1
human A2780 cells M4PTSXBzd2yrZnXyZZRqd25iYYPzZZk> M3K5V|czKGh? MkLBRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczDlfJBz\XO|aX7nJJA2OyCpZX7lJIFnfGW{IEeyJIhzeyCkeTDwdo9tcW[ncnH0bZZmKGG|c3H5MEBKSzVyPUGuNFch|ryP NX3E[|BOOTh2Nkm4NFk>
human SW48 cells NFTtRWpRem:uaX\ldoF1cW:wIHHzd4F6 NUHF[JNkPzJiaB?= NEfHPYVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPXOFgh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZoF{\WRiYYPzZZktKEmFNUC9NU4zKM7:TR?= MnizNVkyOTV6NEW=
human MCF7 cells MULQdo9tcW[ncnH0bY9vKGG|c3H5 MmPJO|IhcA>? NETVV4tCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZoF{\WRiYYPzZZktKEmFNUC9NU4{KM7:TR?= M3zuVlE6OTF3OES1
human U2OS cells M37JfHBzd2yrZnXyZZRqd25iYYPzZZk> NH3FenM4OiCq M4rTNWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iVULPV{Bk\WyuczDlfJBz\XO|aX7nJJA2OyCpZX7lJIFnfGW{IEeyJIhzeyCkeTDwdo9tcW[ncnH0bZZmKGG|c3H5MEBKSzVyPUGuOFkh|ryP NVG4co56OTh2Nkm4NFk>
human COLO205 cells NHLPNJVRem:uaX\ldoF1cW:wIHHzd4F6 M{D0RlczKGh? NWOzUG15SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDDU2xQOjB3IHPlcIx{KGGodHXyJFczKGi{czDifUBtfWOrZnXyZZNmKGKjc3XkJIF{e2G7LDDJR|UxRTFwNTFOwG0> M3vnd|E6OTF3OES1
human OVCAR8 cells M3nD[XBzd2yrZnXyZZRqd25iYYPzZZk> NUm3[otoPzJiaB?= NXnMWnJySW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBxPTNiZHXmbYNq\W62IHj1cYFvKE:YQ1HSPEBk\WyuczDh[pRmeiB5MjDodpMh[nlicILvcIln\XKjdHn2[UBie3OjeTygTWM2OD1zLkW2JO69VQ>? NWjWcmRMOTh2Nkm4NFk>
human L363 cells M4HKUXBzd2yrZnXyZZRqd25iYYPzZZk> NWfwRoZsPzJiaB?= NUfrTWJjSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMN|Y{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIJie2WmIHHzd4F6NCCLQ{WwQVEvPiEQvF2= NFriPZMyQTFzNUi0OS=>
human NHDF cells M4rDUHBzd2yrZnXyZZRqd25iYYPzZZk> Mk\3O|IhcA>? M1rqW2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTljESkBk\WyuczDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDiZZNm\CCjc4PhfUwhUUN3ME2xMlYh|ryP MVKxPVEyPTh2NR?=
human NCI-H929 cells M1vwZXBzd2yrZnXyZZRqd25iYYPzZZk> M3PmU|czKGh? NYXKSFJnSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDl{OTDj[YxteyCjZoTldkA4OiCqcoOgZpkhdHWlaX\ldoF{\SCkYYPl[EBie3OjeTygTWM2OD1zLkig{txO MnPSNVkyOTV6NEW=
human SF539 cells MXPQdo9tcW[ncnH0bY9vKGG|c3H5 NWDZb4hyPzJiaB?= MlviRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVRkWzPUBk\WyuczDlfJBz\XO|aX7nJJA2OyCpZX7lJIFnfGW{IEeyJIhzeyCkeTDwdo9tcW[ncnH0bZZmKGG|c3H5MEBKSzVyPUKuN|Qh|ryP M4PaWFE5PDZ7OEC5
human SW480 cells MkH6VJJwdGmoZYLheIlwdiCjc4PhfS=> NHTWcWo4OiCq M3\4TmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgdFU{KGSnZnnjbYVvfCCqdX3hckBUXzR6MDDj[YxteyCjZoTldkA4OiCqcoOgZpkheHKxbHnm[ZJifGm4ZTDhd5NigSxiSVO1NF0zNjZ5IN88US=> NIHHOIwyQDR4OUiwPS=>
human NCI60 cells Mk\XVJJwdGmoZYLheIlwdiCjc4PhfS=> M1fncmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJOlAh[2WubIOsJGlEPTB;Mz6xJO69VQ>? NEnaTXEyQDR4OUiwPS=>
human Jurkat cells MUnQdo9tcW[ncnH0bY9vKGG|c3H5 MnPWO|IhcA>? MVfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IIC1N{Bl\W[rY3nlcpQhcHWvYX6gTpVzc2G2IHPlcIx{KGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVMvOiEQvF2= Mo\4NVg1Pjl6MEm=
human HCT15 cells NHPybVVRem:uaX\ldoF1cW:wIHHzd4F6 Mm[yO|IhcA>? M4L3R2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVUh[2WubIOg[ZhxemW|c3nu[{BxPTNiZ3Xu[UBi\nSncjC3NkBpenNiYomgdJJwdGmoZYLheIl3\SCjc4PhfUwhUUN3ME2zMlgyKM7:TR?= M3jTOVE5PDZ7OEC5
human OPM2 cells MWnQdo9tcW[ncnH0bY9vKGG|c3H5 MlLyO|IhcA>? NH3Te5NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF;QUVIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHz1Z4ln\XKjc3WgZoF{\WRiYYPzZZktKEmFNUC9OE42KM7:TR?= M3vK[lE6OTF3OES1
human HT-29 cells NH\Kc|ZRem:uaX\ldoF1cW:wIHHzd4F6 NEL6dm84OiCq NXfWOlM1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgcJVkcW[ncnHz[UBj[XOnZDDhd5NigSxiSVO1NF02KM7:TR?= NEXEcW0yQTFzNUi0OS=>
human K562 cells NGDZRpRRem:uaX\ldoF1cW:wIHHzd4F6 NGL0Snc4OiCq M{WxfGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgdFU{KGSnZnnjbYVvfCCqdX3hckBMPTZ{IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD13Lki3JO69VQ>? NU\XXIVIOTh2Nkm4NFk>
U937 cells MVfGeY5kfGmxbjDhd5NigQ>? MmnsTY5pcWKrdHnvckBw\iCWTl\hcJBp[SCycn;keYN1cW:wIHnuJHU6OzdiY3XscJMtKEmFNUC9NVkh|ryP M3vT[|E4PDhyME[0
human HeLa cells MnPOSpVv[3Srb36gZZN{[Xl? M3fOeFUh|ryP NWjlVWpjOjRiaB?= NFnVdXJKdmS3Y4Tpc44hd2ZiYYDvdJRwe2m|IHnuJIh2dWGwIFjlUIEh[2WubIOgZZN{\XO|ZXSgZZMh[XCyZXHyZY5k\SCxZjDQRXJRKGG2IEWgeW0h[W[2ZYKgNlQhcHK| M4njR|E5PDZ7OEC5
NHDF M1vSU2Z2dmO2aX;uJIF{e2G7 MoH3OUDPxE1? Mn\KNVYhcA>? M1PUd2lv\HWldHnvckBw\iClZXzsJIN6[2ynIHHydoV{fCCrbjD0bJlucWSrbnWg[IVncWOrZX70JG5JTEZiYYPz[ZN{\WRiYYOgSG5CKHO7boTo[ZNqeyCrbjDTMZBp[XOnIHH0JFUhfU1iYX\0[ZIhOT[qcoOgSmFEWyCjbnHsfZNqeyCrbjDwdoV{\W6lZTDv[kB{\XK3bR?= NH\uSGcyQDR4OUiwPS=>

... 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
  • 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