2. Cell Cycle/DNA Damage
  3. CDK
  4. AZD-5438

AZD-5438 

Cat. No.: HY-10012 Purity: 99.85%
COA Handling Instructions

AZD-5438 est un inhibiteur puissant de CDK1, de CDK2 et de CDK9, avec IC50s de 16 nM, 6 nM et 20 nM dans des tests sans cellules, respectivement. AZD-5438 montre moins d'activité inhibitrice contre GSK3β, CDK5 et CDK6.

AZD-5438 ist ein potenter CDK1, CDK2, and CDK9-Inhibitor mit IC50s von 16 nM, 6 nM bzw. 20 nM in zellfreien Assays. AZD-5438 zeigt weniger Hemmaktivität gegen GSK3β, CDK5 und CDK6.

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 .

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

AZD-5438 Chemical Structure

AZD-5438 Chemical Structure

CAS No. : 602306-29-6

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 87 In-stock
Solution
10 mM * 1 mL in DMSO USD 87 In-stock
Solid
10 mg USD 79 In-stock
50 mg USD 238 In-stock
100 mg USD 422 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 10 publication(s) in Google Scholar

AZD-5438 Related Antibodies

Top Publications Citing Use of Products

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

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 [1].

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)

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.

AZD-5438 Related Antibodies
In Vivo

AZD5438 (50 mg/kg twice daily or 75 mg/kg, p.o.) inhibits human tumor xenograft growth. In vivo, AZD5438 reduces the proportion of actively cycling cells. Further pharmacodynamic analysis of AZD5438-treated SW620 xenografts shows that efficacious doses of AZD5438 (>40% tumor growth inhibition) maintains suppression of biomarkers, such as phospho-pRbSer249/Thr252, for up to 16 hours following a single oral dose[1].

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

371.46

Appearance

Solid

Formula

C18H21N5O2S
CAS No.
SMILES

O=S(C1=CC=C(NC2=NC(C3=CN=C(N3C(C)C)C)=CC=N2)C=C1)(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 1 year
-20°C 6 months
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (269.21 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

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

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.85%

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

Handling Instructions (2659 KB)
References
Cell Assay
[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 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[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 has not independently confirmed the accuracy of these methods. They are for reference only.
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

AZD-5438 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.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
AZD-5438
Cat. No.:
HY-10012
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.