2. Cell Cycle/DNA Damage
  3. CDK
  4. AZD8421

AZD8421 is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer.

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AZD8421 Chemical Structure

AZD8421 Chemical Structure

CAS No. : 3047321-53-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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10 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

AZD8421 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

  • Purity & Documentation

  • References

  • Customer Review

Description

AZD8421 is a selective CDK2 inhibitor (IC50 = 9 nM) as well as achieving CDK family selectivity in cells versus key off-targets (CDK1, CDK4/6, CDK9), AZD8421 had no significant kinase inhibition outside the CDK family. AZD8421 inhibits cancer cell proliferation by inhibiting pRB phosphorylation, inducing cell cycle arrest in G1/S phase and senescence. AZD8421 can be studied in research for breast cancer and ovarian cancer[1].

IC50 & Target

CDK2[1]
In Vitro

AZD8421 inhibits endogenous phospho-substrate at 58nM with >327-fold selectivity over CDK9 phospho-substrate pSer2 of RNAPIl (>19.2 μM)[1].
AZD8421 potently inhibites cell proliferation (69nM, OVCAR3), correlates with inhibition of pRB, arrest in G1/S phase of the cell cycle and induction of senescence in a CCNE1 amplified cell line[1].
AZD8421 (Compound CDK2i) (500 nM, 72 h) effectively downregulates p130 in combination with Abemaciclib (HY-16297) (50 nM) in p53KO cells[2].
AZD8421 (500 nM, 8 d) blocks cell-cycle re-entry upon drug withdrawal in combination with Abemaciclib in p53KO cells[2].
AZD8421 (500 nM, 10 d) enables long-term growth suppression of p53KO cells when combined with Abemaciclib, which is associated with potent induction of SA-β-Gal expression[2].
AZD8421 (500 nM, 6 d) suppresses the phosphorylation of both Rb and p130, long-term growth, growth after withdrawal of the drug, and induces SA-β-Gal activity when combined with Abemaciclib in HR+/HER2- p53 mutant primary breast cancer cell line and PD BC line #5[2].

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

AZD8421 Related Antibodies
In Vivo

AZD8421 potently suppresses phosphorylation of Rb, and demonstrated robust monotherapy and CDK4/6i combination activity in breast and ovarian in vivo models[1].
AZD8421 shows robust monotherapy activity in a CCNE1 amplified ovarian model OVCAR3 with regressions seen with monotherapy and in combination with Palbociclib (HY-50767)[1].
AZD8421 (100 mg/kg, p.o., 5 d) markedly reduces MKI67, p130 phosphorylation, E2F1, and cyclin A2 levels in combination with Ribociclib (HY-15777) (25 mg/kg) compared to single agents[2].

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

440.56

Formula

C18H32N8O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCN1C=NC2=C1N=C(N[C@@H](CC)[C@@H](C)O)N=C2N[C@@H]3CN(S(=O)(NCC)=O)CC3
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 : 100 mg/mL (226.98 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 2.2698 mL 11.3492 mL 22.6984 mL
5 mM 0.4540 mL 2.2698 mL 4.5397 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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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

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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: ≥ 2.5 mg/mL (5.67 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 (5.67 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.
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.
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.
Purity & Documentation

Purity: 99.60%

SDS (251 KB)

COA (252 KB) HNMR (154 KB) RP-HPLC (172 KB) LCMS (109 KB)

Handling Instructions (2659 KB)
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. 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 2.2698 mL 11.3492 mL 22.6984 mL 56.7460 mL
5 mM 0.4540 mL 2.2698 mL 4.5397 mL 11.3492 mL
10 mM 0.2270 mL 1.1349 mL 2.2698 mL 5.6746 mL
15 mM 0.1513 mL 0.7566 mL 1.5132 mL 3.7831 mL
20 mM 0.1135 mL 0.5675 mL 1.1349 mL 2.8373 mL
25 mM 0.0908 mL 0.4540 mL 0.9079 mL 2.2698 mL
30 mM 0.0757 mL 0.3783 mL 0.7566 mL 1.8915 mL
40 mM 0.0567 mL 0.2837 mL 0.5675 mL 1.4186 mL
50 mM 0.0454 mL 0.2270 mL 0.4540 mL 1.1349 mL
60 mM 0.0378 mL 0.1892 mL 0.3783 mL 0.9458 mL
80 mM 0.0284 mL 0.1419 mL 0.2837 mL 0.7093 mL
100 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5675 mL
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AZD8421 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:

AZD84213047321-53-6AZD 8421AZD-8421CDKCyclin dependent kinasepRB phosphorylationcell cycle arrestcellular senescencedrug-resistant breast cancer cellsInhibitorinhibitorinhibit

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