Cat. No.: HY-13461

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PHA-767491

(Synonyms: CAY10572)

5 Cited Publications

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Based on 5 publication(s) in Google Scholar

PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC₅₀s of 10 nM and 34 nM, respectively.

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Pureté: 99.97%
CAS No.: 845714-00-3
Formule: C₁₂H₁₁N₃O
Masse moléculaire:213.24

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PHA-767491 Chemical Structure

CAS No.: 845714-00-3

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC₅₀s of 10 nM and 34 nM, respectively.

IC₅₀ & Target^[4]

CDK9

34 nM (IC₅₀)

CDK2

240 nM (IC₅₀)

CDK1

250 nM (IC₅₀)

CDK5

460 nM (IC₅₀)

GSK3-β

220 nM (IC₅₀)

Mk2

470 nM (IC₅₀)

Plk1

980 nM (IC₅₀)

Chk2

1100 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform CDK :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	1.07 μM Compound: 1, PHA-767491	Antiproliferative activity against human A2780 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human A2780 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
A2780	IC₅₀	1.1 μM Compound: 1	Antiproliferative activity against human A2780 cells after 72 hrs Antiproliferative activity against human A2780 cells after 72 hrs	[PMID: 18201066]
A2780	IC₅₀	1.1 μM Compound: 1	Antiproliferative activity against human A2780 cells after 72 hrs by luciferase based assay Antiproliferative activity against human A2780 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
COLO 205	IC₅₀	1.5 μM Compound: 1	Antiproliferative activity against human COLO205 cells after 72 hrs by luciferase based assay Antiproliferative activity against human COLO205 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
COLO 205	IC₅₀	1.54 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human COLO205 cells after 72 hrs Antiproliferative activity against p53 deficient human COLO205 cells after 72 hrs	[PMID: 18469809]
HCT-116	IC₅₀	0.97 μM Compound: 1, PHA-767491	Antiproliferative activity against human HCT116 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human HCT116 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
HCT-15	IC₅₀	3.81 μM Compound: 1, PHA-767491	Antiproliferative activity against human HCT15 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human HCT15 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
HeLa	IC₅₀	1.83 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human HeLa cells after 72 hrs Antiproliferative activity against p53 deficient human HeLa cells after 72 hrs	[PMID: 18469809]
HT-29	IC₅₀	5 μM Compound: 1	Antiproliferative activity against human HT-29 cells after 72 hrs by luciferase based assay Antiproliferative activity against human HT-29 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
Jurkat	IC₅₀	3.2 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human Jurkat cells after 72 hrs by proliferative assay Antiproliferative activity against p53 deficient human Jurkat cells after 72 hrs by proliferative assay	[PMID: 18469809]
K562	IC₅₀	5.87 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human K562 cells after 72 hrs Antiproliferative activity against p53 deficient human K562 cells after 72 hrs	[PMID: 18469809]
L-363	IC₅₀	1.6 μM Compound: 1	Antiproliferative activity against human L363 cells after 72 hrs by luciferase based assay Antiproliferative activity against human L363 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
MCF7	IC₅₀	1.3 μM Compound: 1	Antiproliferative activity against human MCF7 cells after 72 hrs by luciferase based assay Antiproliferative activity against human MCF7 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
MCF7	IC₅₀	1.33 μM Compound: 1, PHA-767491	Antiproliferative activity against human MCF7 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human MCF7 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
NCI-H929	IC₅₀	1.8 μM Compound: 1	Antiproliferative activity against human NCI-H929 cells after 72 hrs by luciferase based assay Antiproliferative activity against human NCI-H929 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
NHDF	IC₅₀	1.58 μM Compound: 1, PHA-767491	Antiproliferative activity against NHDF expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against NHDF expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
NHDF	IC₅₀	1.6 μM Compound: 1	Antiproliferative activity against human NHDF cells after 72 hrs by luciferase based assay Antiproliferative activity against human NHDF cells after 72 hrs by luciferase based assay	[PMID: 19115845]
OPM-2	IC₅₀	4.5 μM Compound: 1	Antiproliferative activity against human OPM2 cells after 72 hrs by luciferase based assay Antiproliferative activity against human OPM2 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
OVCAR-8	IC₅₀	1.56 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human OVCAR8 cells after 72 hrs by proliferative assay Antiproliferative activity against p53 deficient human OVCAR8 cells after 72 hrs by proliferative assay	[PMID: 18469809]
PC-3	IC₅₀	4.59 μM Compound: 1, PHA-767491	Antiproliferative activity against human PC3 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human PC3 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
SF-268	IC₅₀	0.86 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human SF268 cells after 72 hrs Antiproliferative activity against p53 deficient human SF268 cells after 72 hrs	[PMID: 18469809]
SF-539	IC₅₀	2.34 μM Compound: 1, PHA-767491	Antiproliferative activity against human SF539 cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human SF539 cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
SW48	IC₅₀	1.2 μM Compound: 1	Antiproliferative activity against human SW48 cells after 72 hrs by luciferase based assay Antiproliferative activity against human SW48 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
SW480	IC₅₀	2.67 μM Compound: 1, PHA-767491	Antiproliferative activity against p53 deficient human SW480 cells after 72 hrs by proliferative assay Antiproliferative activity against p53 deficient human SW480 cells after 72 hrs by proliferative assay	[PMID: 18469809]
U2OS	IC₅₀	1.49 μM Compound: 1, PHA-767491	Antiproliferative activity against human U2OS cells expressing p53 gene after 72 hrs by proliferative assay Antiproliferative activity against human U2OS cells expressing p53 gene after 72 hrs by proliferative assay	[PMID: 18469809]
U-937	IC₅₀	19 μM Compound: 8	Inhibition of TNFalpha production in U937 cells Inhibition of TNFalpha production in U937 cells	[PMID: 17480064]

In Vitro

PHA-767491 inhibits proliferation in both cell lines with an IC₅₀ of 0.64 µM in HCC1954 cells and 1.3 µM in Colo-205 cells. PHA-767491 is effective DDK inhibitors in vitro, with IC₅₀ values of 18.6 nM. PHA-767491 (2 µM) completely abolishes Mcm2 phosphorylation by 24 hours in HCC1954 cells^[1]. PHA-767491 in combination with 5-FU exhibits much stronger cytotoxicity and induces significant apoptosis manifested by remarkably increased caspase 3 activation and poly(ADP-Ribose) polymerase fragmentation in HCC cells. PHA-767491 directly counteracts the 5-FU-induced phosphorylation of Chk1 and decreases the expression of the anti-apoptotic protein myeloid leukemia cell 1ine^[2]. PHA-767491 (0-10 µM) decreases glioblastoma cell viability in a time- and dose-dependent fashion, with IC₅₀ of approximately 2.5 µM for U87-MG and U251-MG cells. PHA-767491 hydrochloride induces apoptosis in glioblastoma cells, suppresses glioblastoma cell proliferation, cell migration and cell invasion^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PHA-767491 decreases Chk1 phosphorylation and increases in situ cell apoptosis in tumor tissues sectioned from nude mice HCC xenografts^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 845714-00-3
Appearance Solid
Masse moléculaire 213.24
Formule C₁₂H₁₁N₃O
Color Off-white to light yellow
SMILES

O=C1C2=C(NC(C3=CC=NC=C3)=C2)CCN1
Synonyms

CAY10572
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (5)

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Journal Impact Factor

Nat Commun

CDK9 recruits HUWE1 to degrade RARα and offers therapeutic opportunities for cutaneous T-cell lymphoma. [Abstract]

2024 Dec 5;15(1):10594. PMID: 39632829
Autophagy

CDK9 inhibition blocks the initiation of PINK1-PRKN-mediated mitophagy by regulating the SIRT1-FOXO3-BNIP3 axis and enhances the therapeutic effects involving mitochondrial dysfunction in hepatocellular carcinoma. [Abstract]

2022 Aug;18(8):1879-1897. PMID: 34890308
Acta Pharmacol Sin

Novel CDK9 inhibitor oroxylin A promotes wild-type P53 stability and prevents hepatocellular carcinoma progression by disrupting both MDM2 and SIRT1 signaling. [Abstract]

2022 Apr;43(4):1033-1045. PMID: 34188177
Sci Rep

Pre-therapeutic efficacy of the CDK inhibitor dinaciclib in medulloblastoma cells. [Abstract]

2021 Mar 8;11(1):5374. PMID: 33686114
Genes Genomics

CDK9 inhibition triggers MT2A-dependent apoptosis in HCC cells. [Abstract]

2026 Jun;48(6):817-829. PMID: 41954877

Solvant et solubilité

In Vitro:

DMSO : 15.38 mg/mL (72.13 mM; ultrasonic and adjust pH to 2 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.6896 mL

23.4478 mL

46.8955 mL

5 mM

0.9379 mL

4.6896 mL

9.3791 mL

10 mM

0.4690 mL

2.3448 mL

4.6896 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.54 mg/mL (7.22 mM); Clear solution

This protocol yields a clear solution of ≥ 1.54 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.4 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.54 mg/mL (7.22 mM); Clear solution

This protocol yields a clear solution of ≥ 1.54 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.4 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.54 mg/mL (7.22 mM); Clear solution

This protocol yields a clear solution of ≥ 1.54 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (15.4 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[1]

20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 µCi (γ)-³²P ATP and 1.5 µM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl₂, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. ³²P-labeled bands are quantified using ImageJ and the IC₅₀ values are calculated using GraphPad.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC₅₀ values are calculated using the GraphPad software. For assays in six well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 µL of this suspension is mixed with 30 µL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Sasi NK, et al. The potent Cdc7-Dbf4 (DDK) kinase inhibitor XL413 has limited activity in many cancer cell lines and discovery of potential new DDK inhibitor scaffolds. PLoS One. 2014 Nov 20;9(11):e113300. [Content Brief]

[2]. Li W, et al. Dual Inhibition of Cdc7 and Cdk9 by PHA-767491 Suppresses Hepatocarcinoma Synergistically with 5-Fluorouracil. Curr Cancer Drug Targets. 2015;15(3):196-204. [Content Brief]

[3]. Erbayraktar Z, et al. Cell division cycle 7-kinase inhibitor PHA-767491 hydrochloride suppresses glioblastoma growth and invasiveness. Cancer Cell Int. 2016 Nov 18;16:88. [Content Brief]

[4]. Montagnoli A, et al. A Cdc7 kinase inhibitor restricts initiation of DNA replication and has antitumor activity. Nat Chem Biol. 2008 Jun;4(6):357-65. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.6896 mL	23.4478 mL	46.8955 mL	117.2388 mL
	5 mM	0.9379 mL	4.6896 mL	9.3791 mL	23.4478 mL
	10 mM	0.4690 mL	2.3448 mL	4.6896 mL	11.7239 mL
	15 mM	0.3126 mL	1.5632 mL	3.1264 mL	7.8159 mL
	20 mM	0.2345 mL	1.1724 mL	2.3448 mL	5.8619 mL
	25 mM	0.1876 mL	0.9379 mL	1.8758 mL	4.6896 mL
	30 mM	0.1563 mL	0.7816 mL	1.5632 mL	3.9080 mL
	40 mM	0.1172 mL	0.5862 mL	1.1724 mL	2.9310 mL
	50 mM	0.0938 mL	0.4690 mL	0.9379 mL	2.3448 mL
	60 mM	0.0782 mL	0.3908 mL	0.7816 mL	1.9540 mL

Keywords

PHA-767491

5 Cited Publications

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PHA-767491

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) PHA-767491

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PHA-767491

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Blood Cancer Compound Library

Cancer Stem Cells Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) PHA-767491

Voir tous les produits spécifiques à Isoform CDK

Activité biologique

Chemical Information

Publications (5)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

PHA-767491 Related Classifications

HY-13461 Related Classifications