2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. PHA-767491 hydrochloride

PHA-767491 hydrochloride  (Synonyms: CAY-10572 hydrochloride)

Cat. No.: HY-13461A Purity: 98.06%
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PHA-767491 hydrochloride 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 hydrochloride Chemical Structure

PHA-767491 hydrochloride Chemical Structure

CAS No. : 942425-68-5

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10 mM * 1 mL in DMSO
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of PHA-767491 hydrochloride:

PHA-767491 hydrochloride Related Antibodies

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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 hydrochloride 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)

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.

PHA-767491 hydrochloride Related Antibodies
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

249.70

Formula

C12H12ClN3O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(NC(C3=CC=NC=C3)=C2)CCN1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (200.24 mM; Need ultrasonic)

DMSO : 17.33 mg/mL (69.40 mM; Need ultrasonic and warming; 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 4.0048 mL 20.0240 mL 40.0481 mL
5 mM 0.8010 mL 4.0048 mL 8.0096 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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 mg/mL (4.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 1 mg/mL (4.00 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (200.24 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References
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

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 (sealed storage, away from moisture). 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 / H2O 1 mM 4.0048 mL 20.0240 mL 40.0481 mL 100.1201 mL
5 mM 0.8010 mL 4.0048 mL 8.0096 mL 20.0240 mL
10 mM 0.4005 mL 2.0024 mL 4.0048 mL 10.0120 mL
15 mM 0.2670 mL 1.3349 mL 2.6699 mL 6.6747 mL
20 mM 0.2002 mL 1.0012 mL 2.0024 mL 5.0060 mL
25 mM 0.1602 mL 0.8010 mL 1.6019 mL 4.0048 mL
30 mM 0.1335 mL 0.6675 mL 1.3349 mL 3.3373 mL
40 mM 0.1001 mL 0.5006 mL 1.0012 mL 2.5030 mL
50 mM 0.0801 mL 0.4005 mL 0.8010 mL 2.0024 mL
60 mM 0.0667 mL 0.3337 mL 0.6675 mL 1.6687 mL
H2O 80 mM 0.0501 mL 0.2503 mL 0.5006 mL 1.2515 mL
100 mM 0.0400 mL 0.2002 mL 0.4005 mL 1.0012 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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PHA-767491 hydrochloride 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-767491942425-68-5CAY-10572PHA767491PHA 767491CAY10572CAY 10572CDKApoptosisCyclin dependent kinaseInhibitorinhibitorinhibit

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