Reagenzien und Instrumente für die Immunologie Zellbiologie und Molekularbiologie

AZD-5438 [602306-29-6]

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Katalog-Nummer HY-10012-1ml

Size : 10mM/1mL

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AZD-5438 | CDK1/2/9 Inhibitor | MedChemExpress

AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC₅₀s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 .

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AZD-5438 Chemische Struktur

CAS. Nr. : 602306-29-6

Kundenbewertung

Based on 12 publication(s) in Google Scholar

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle CDK Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

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

Biologische Aktivität
Protokoll
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

IC₅₀ & Target^[1]

cdk2-cyclin E

6 nM (IC₅₀)

cdk2-cyclin A

45 nM (IC₅₀)

cdk5-p25

14 nM (IC₅₀)

cdk1-cyclin B1

16 nM (IC₅₀)

cdk9-cyclin T

20 nM (IC₅₀)

cdk6-cyclin D3

21 nM (IC₅₀)

cdk4-cyclin D1

449 nM (IC₅₀)

cdk7-cyclin H

821 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	0.47 μM Compound: AZD5438	Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay	[PMID: 31254921]
HeLa	IC₅₀	0.73 μM Compound: AZD5438	Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay	[PMID: 31254921]
HeLa	IC₅₀	1.2 μM Compound: 6; MMV676604	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay	[PMID: 30647879]
LoVo	IC₅₀	0.63 μM Compound: 6c, AZD-5438	Antiproliferative activity against human LoVo cells assessed as BrdU incorporation after 48 hrs Antiproliferative activity against human LoVo cells assessed as BrdU incorporation after 48 hrs	[PMID: 18815031]
LoVo	IC₅₀	0.8 μM Compound: 1, AZD-5438	Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs	[PMID: 18996007]
LoVo	IC₅₀	0.8 μM Compound: 6	Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs	[PMID: 18986805]
MCF7	IC₅₀	10.67 μM Compound: AZD5438	Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay	[PMID: 31254921]
MDA-MB-231	IC₅₀	7.2 μM Compound: AZD5438	Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay	[PMID: 31254921]
PC-3	IC₅₀	0.36 μM Compound: AZD5438	Antiproliferative activity against human PC3 cells incubated for 48 hrs by MTT assay Antiproliferative activity against human PC3 cells incubated for 48 hrs by MTT assay	[PMID: 31254921]

In Vitro

AZD5438 potently inhibits the kinase activity of cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, p25-cdk5, cyclin D3-cdk6, and cyclin T-cdk9 (IC₅₀, 6, 45, 16, 21, and 20 nM, respectively). AZD5438 potently inhibits the kinase activity of cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, p25-cdk5, cyclin D3-cdk6, and cyclin T-cdk9 (IC₅₀, 6, 45, 16, 21, and 20 nM, respectively). In common with many other cdk inhibitors, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β in vitro (IC₅₀, 14 and 17 nM, respectively)^[1]. AZD5438 significantly augments cellular radiosensitivity in NSCLC cells. Combined treatment with AZD5438 and irradiation also enhances tumor growth delay, with an enhancement factor ranging from 1.2-1.7^[2].

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (269.21 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	2.6921 mL	13.4604 mL	26.9208 mL
5 mM	0.5384 mL	2.6921 mL	5.3842 mL
10 mM	0.2692 mL	1.3460 mL	2.6921 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molaritätsrechner
Verdünnungsrechner

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.5 mg/mL (6.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Reinheit & Dokumentation

Purity: 99.85%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (251 KB) HNMR (132 KB) RP-HPLC (126 KB)

Handling Instructions (2659 KB)

Verweise

[1]. Byth KF, et al. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol Cancer Ther. 2009 Jul;8(7):1856-66. Epub 2009 Jun 9. [Content Brief]

[2]. Raghavan P, et al. AZD5438, an Inhibitor of Cdk1, 2, and 9, Enhances the Radiosensitivity of Non-Small Cell Lung Carcinoma Cells. Int J Radiat Oncol Biol Phys. 2012 Jul 12. [Content Brief]

Zellassay ^[1]	AZD5438 is tested against solid tumor cell lines as previously described. Briefly, cells are incubated for 48 h with AZD5438 at a range of concentrations. At the end of incubation, the cells are pulsed with 5-bromo-2'-deoxyuridine (BrdUrd) and the amount of DNA synthesis is measured. The IC₅₀ for inhibition of proliferation is specifically determined independently of cell death. Multiple myeloma cell lines are seeded into 96-well plates in RPMI 1640 supplemented with 10% FCS and glutamine and dosed with AZD5438 for 72 h. Cell growth is measured using AlamarBlue and GI₅₀ values are calculated with reference to pretreatment control values. MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Tierverwaltung ^[1]	All human tumor xenografts except HX147 are established by s.c. injecting 100 μL of tumor cells (between 1×10⁶ and 1×10⁷ cells mixed 1:1 with Matrigel). HX147 tumors are derived from fragment implants (1 mm³ pieces) from tumors taken from mice initially implanted s.c. with 1×10⁷ cells. These tumor fragments are passaged in mice thrice before implant for antitumor work. Tumors are measured up to three times per week with calipers, tumor volumes are calculated, and the data are plotted as geometric mean for each group versus time, as previously described. Animals are randomized into treatment groups (typically n=10) when tumors reach a mean size of approximately >0.2 cm³ and >0.5 cm³ for mice and rats, respectively. AZD5438 is prepared in hydroxy-propyl-methyl-cellulose. Animals are given either AZD5438 (37.5-75 mg/kg) or vehicle control once or twice daily by oral gavage for appr 3 wk in each case. Tumor volume and percentage tumor growth inhibition (% TGI) are calculated as described previously. Statistical analysis of any change in tumor volume is carried out using a standard t test (P<0.05 is considered to be statistically significant). MCE hat die Genauigkeit dieser Methoden nicht unabhängig bestätigt. Sie dienen nur als Referenz.
Verweise	[1]. Byth KF, et al. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol Cancer Ther. 2009 Jul;8(7):1856-66. Epub 2009 Jun 9. [Content Brief] [2]. Raghavan P, et al. AZD5438, an Inhibitor of Cdk1, 2, and 9, Enhances the Radiosensitivity of Non-Small Cell Lung Carcinoma Cells. Int J Radiat Oncol Biol Phys. 2012 Jul 12. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6921 mL	13.4604 mL	26.9208 mL	67.3020 mL
	5 mM	0.5384 mL	2.6921 mL	5.3842 mL	13.4604 mL
	10 mM	0.2692 mL	1.3460 mL	2.6921 mL	6.7302 mL
	15 mM	0.1795 mL	0.8974 mL	1.7947 mL	4.4868 mL
	20 mM	0.1346 mL	0.6730 mL	1.3460 mL	3.3651 mL
	25 mM	0.1077 mL	0.5384 mL	1.0768 mL	2.6921 mL
	30 mM	0.0897 mL	0.4487 mL	0.8974 mL	2.2434 mL
	40 mM	0.0673 mL	0.3365 mL	0.6730 mL	1.6825 mL
	50 mM	0.0538 mL	0.2692 mL	0.5384 mL	1.3460 mL
	60 mM	0.0449 mL	0.2243 mL	0.4487 mL	1.1217 mL
	80 mM	0.0337 mL	0.1683 mL	0.3365 mL	0.8413 mL
	100 mM	0.0269 mL	0.1346 mL	0.2692 mL	0.6730 mL

AZD-5438 Related Classifications

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Keywords:

AZD-5438602306-29-6AZD5438AZD 5438CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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AZD-5438 [602306-29-6]

Katalog-Nummer HY-10012-1ml

Contact local distributor :

Marke : MedChemExpress

Contact local distributor :

Kundenbewertung

AZD-5438 Related Antibodies

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle CDK Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Protokoll

Reinheit & Dokumentation

Verweise

Kundenbewertung

AZD-5438 Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

AZD-5438 Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

Kundenbewertung

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