PHA-767491 (Synonyms: CAY10572)

Name: PHA-767491
Brand: MedChemExpress
SKU: HY-13461
Rating: 5.0 (3 reviews)

Cat. No.: HY-13461 Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

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

For research use only. We do not sell to patients.

PHA-767491 Chemical Structure

CAS No. : 845714-00-3

Size	Price	Stock	Quantity
5 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 125	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of PHA-767491:

PHA-767491 hydrochloride In-stock

3 Publications Citing Use of MCE PHA-767491

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View All CDK Isoform Specific Products:

View All Isoforms

CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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)

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 by luciferase based assay Antiproliferative activity against human A2780 cells after 72 hrs by luciferase based assay	[PMID: 19115845]
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]
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]

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.

Molecular Weight

213.24

Formula

C₁₂H₁₁N₃O

CAS No.

845714-00-3

Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL (117.24 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.85%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (246 KB) HNMR (249 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[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]

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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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
	80 mM	0.0586 mL	0.2931 mL	0.5862 mL	1.4655 mL
	100 mM	0.0469 mL	0.2345 mL	0.4690 mL	1.1724 mL

PHA-767491 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PHA-767491845714-00-3CAY10572PHA767491PHA 767491CAY 10572CAY-10572CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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PHA-767491 (Synonyms: CAY10572)

Customer Review

Other Forms of PHA-767491:

PHA-767491 Related Antibodies

3 Publications Citing Use of MCE PHA-767491

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All CDK Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

PHA-767491 Related Antibodies

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Complete Stock Solution Preparation Table

PHA-767491 Related Classifications

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