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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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 NFjnVnRRem:uaX\ldoF1cW:wIHHzd4F6 NIjZ[VU4OiCq NXq3NVd[SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBxPTNiZHXmbYNq\W62IHj1cYFvKFOIMk[4JINmdGy|IHHmeIVzKDd{IHjyd{whUUN3ME2wMlg3KM7:TR?= Mn76NVg1Pjl6MEm=
human HCT116 cells NUDtXI5KWHKxbHnm[ZJifGmxbjDhd5NigQ>? Ml3OO|IhcA>? NV7ZT4hsSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh\XiycnXzd4lv\yCyNUOg[4Vv\SCjZoTldkA4OiCqcoOgZpkheHKxbHnm[ZJifGm4ZTDhd5NigSxiSVO1NF0xNjl5IN88US=> NXfHUJNKOTh2Nkm4NFk>
human HCT16 cells M4XHUXBzd2yrZnXyZZRqd25iYYPzZZk> MX:3NkBp MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEG2JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCudXPp[oVz[XOnIHLhd4VlKGG|c3H5MEBKSzVyPUGg{txO NX7LbJNTOTlzMUW4OFU>
human SW403 cells MYLQdo9tcW[ncnH0bY9vKGG|c3H5 NFTXW204OiCq MoDuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVV{SwN{Bk\WyuczDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDiZZNm\CCjc4PhfUwhUUN3ME2xJO69VQ>? NET6TVMyQTFzNUi0OS=>
human A2780 cells M{jPfHBzd2yrZnXyZZRqd25iYYPzZZk> MV[3NkBp MnfORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDMke4NEBk\WyuczDlfJBz\XO|aX7nJJA2OyCpZX7lJIFnfGW{IEeyJIhzeyCkeTDwdo9tcW[ncnH0bZZmKGG|c3H5MEBKSzVyPUGuNFch|ryP MWGxPFQ3QThyOR?=
human SW48 cells NYOxbFRRWHKxbHnm[ZJifGmxbjDhd5NigQ>? NHPWXWk4OiCq MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOZNEigZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KGy3Y3nm[ZJie2ViYnHz[YQh[XO|YYmsJGlEPTB;MT6yJO69VQ>? NVy5cYs4OTlzMUW4OFU>
human MCF7 cells M2fK[3Bzd2yrZnXyZZRqd25iYYPzZZk> NF\LdJM4OiCq NVfhT5h6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIJie2WmIHHzd4F6NCCLQ{WwQVEvOyEQvF2= NWrlZmtIOTlzMUW4OFU>
human U2OS cells Mor4VJJwdGmoZYLheIlwdiCjc4PhfS=> MXG3NkBp MVHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFV{T2OgZ4VtdHNiZYjwdoV{e2mwZzDwOVMh\2WwZTDh[pRmeiB5MjDodpMh[nlicILvcIln\XKjdHn2[UBie3OjeTygTWM2OD1zLkS5JO69VQ>? MoDnNVg1Pjl6MEm=
human COLO205 cells NV[xfJZkWHKxbHnm[ZJifGmxbjDhd5NigQ>? NUP4S4NpPzJiaB?= MnrQRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCFT1zPNlA2KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIJie2WmIHHzd4F6NCCLQ{WwQVEvPSEQvF2= NI\2TnkyQTFzNUi0OS=>
human OVCAR8 cells M4PtXnBzd2yrZnXyZZRqd25iYYPzZZk> NX34bYFnPzJiaB?= MXfBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IIC1N{Bl\W[rY3nlcpQhcHWvYX6gU3ZESVJ6IHPlcIx{KGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVEvPTZizszN NHr0NYkyQDR4OUiwPS=>
human L363 cells NHnDUW9Rem:uaX\ldoF1cW:wIHHzd4F6 MVq3NkBp M2n0bWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTEO2N{Bk\WyuczDh[pRmeiB5MjDodpMh[nlibIXjbYZmemG|ZTDiZZNm\CCjc4PhfUwhUUN3ME2xMlYh|ryP MnfyNVkyOTV6NEW=
human NHDF cells NFrP[3JRem:uaX\ldoF1cW:wIHHzd4F6 M1\meVczKGh? MWPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6KRF[gZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KGy3Y3nm[ZJie2ViYnHz[YQh[XO|YYmsJGlEPTB;MT62JO69VQ>? MlfjNVkyOTV6NEW=
human NCI-H929 cells NGHaTlZRem:uaX\ldoF1cW:wIHHzd4F6 MknWO|IhcA>? MU\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3IPVI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDseYNq\mW{YYPlJIJie2WmIHHzd4F6NCCLQ{WwQVEvQCEQvF2= M{e2XVE6OTF3OES1
human SF539 cells NVv0b5lpWHKxbHnm[ZJifGmxbjDhd5NigQ>? MVe3NkBp M1XFOWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1[1N|kh[2WubIOg[ZhxemW|c3nu[{BxPTNiZ3Xu[UBi\nSncjC3NkBpenNiYomgdJJwdGmoZYLheIl3\SCjc4PhfUwhUUN3ME2yMlM1KM7:TR?= MWexPFQ3QThyOR?=
human SW480 cells NX76OIY{WHKxbHnm[ZJifGmxbjDhd5NigQ>? NVvJelBSPzJiaB?= M376W2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgdFU{KGSnZnnjbYVvfCCqdX3hckBUXzR6MDDj[YxteyCjZoTldkA4OiCqcoOgZpkheHKxbHnm[ZJifGm4ZTDhd5NigSxiSVO1NF0zNjZ5IN88US=> M{LFbFE5PDZ7OEC5
human NCI60 cells M{DKOHBzd2yrZnXyZZRqd25iYYPzZZk> NXPq[JF4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2k3OCClZXzsd{whUUN3ME2zMlEh|ryP NXHFXZN[OTh2Nkm4NFk>
human Jurkat cells M2rLbXBzd2yrZnXyZZRqd25iYYPzZZk> NGfXcpI4OiCq M17UV2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgdFU{KGSnZnnjbYVvfCCqdX3hckBLfXKtYYSgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KHC{b3zp[oVz[XSrdnWgZZN{[XluIFnDOVA:Oy5{IN88US=> M3rxN|E5PDZ7OEC5
human HCT15 cells MXTQdo9tcW[ncnH0bY9vKGG|c3H5 MYK3NkBp NXKwUJk1SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyPSClZXzsd{BmgHC{ZYPzbY5oKHB3MzDn[Y5mKGGodHXyJFczKGi{czDifUBxem:uaX\ldoF1cX[nIHHzd4F6NCCLQ{WwQVMvQDFizszN NH[4[ZMyQDR4OUiwPS=>
human OPM2 cells M2PONXBzd2yrZnXyZZRqd25iYYPzZZk> NFfDNI84OiCq MUPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE:STUKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KGy3Y3nm[ZJie2ViYnHz[YQh[XO|YYmsJGlEPTB;ND61JO69VQ>? NILwZVQyQTFzNUi0OS=>
human HT-29 cells MWDQdo9tcW[ncnH0bY9vKGG|c3H5 MYK3NkBp NYPHNZFbSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgcJVkcW[ncnHz[UBj[XOnZDDhd5NigSxiSVO1NF02KM7:TR?= NH\LVmwyQTFzNUi0OS=>
human K562 cells MnXpVJJwdGmoZYLheIlwdiCjc4PhfS=> M1zyUVczKGh? NUfJeWYzSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBxPTNiZHXmbYNq\W62IHj1cYFvKEt3NkKgZ4VtdHNiYX\0[ZIhPzJiaILzMEBKSzVyPUWuPFch|ryP M3KxS|E5PDZ7OEC5
U937 cells NWnq[nQ6TnWwY4Tpc44h[XO|YYm= M1LqZWlvcGmkaYTpc44hd2ZiVF7GZYxxcGFicILv[JVkfGmxbjDpckBWQTN5IHPlcIx{NCCLQ{WwQVE6KM7:TR?= MnjWNVc1QDByNkS=
human HeLa cells MYDGeY5kfGmxbjDhd5NigQ>? MkPiOUDPxE1? MUiyOEBp M{\YOmlv\HWldHnvckBw\iCjcH;weI9{cXNiaX6gbJVu[W5iSHXMZUBk\WyuczDhd5Nme3OnZDDhd{BieHCnYYLhcoNmKG:oIGDBVnAh[XRiNTD1UUBi\nSncjCyOEBpenN? NULlWIhuOTh2Nkm4NFk>
NHDF MXTGeY5kfGmxbjDhd5NigQ>? Ml;zOUDPxE1? NF;VWpcyPiCq MkC2TY5lfWO2aX;uJI9nKGOnbHygZ5lkdGViYYLy[ZN1KGmwIITofY1q\GmwZTDk[YZq[2mnboSgUmhFTiCjc4Pld5Nm\CCjczDEUmEhe3mwdHjld4l{KGmwIGOtdIhie2ViYYSgOUB2VSCjZoTldkAyPmi{czDGRWNUKGGwYXz5d4l{KGmwIIDy[ZNmdmOnIH;mJJNmenWv NWS4PY9tOTh2Nkm4NFk>

... 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 individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 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 249.7


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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID