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Chemical Structure| 1620576-64-8 Chemical Structure| 1620576-64-8

Structure of AZD-8835
CAS No.: 1620576-64-8

Chemical Structure| 1620576-64-8

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AZD8835 is an effective selective PI3Kα and PI3Kδ inhibitor with IC50 values of 6.2 and 5.7 nM, respectively.

Synonyms: AZD-8835

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Product Details of AZD-8835

CAS No. :1620576-64-8
Formula : C22H31N9O3
M.W : 469.54
SMILES Code : CC(C)(C1=NN=C(O1)C2=NC(C3=NC(C4CCN(CC4)C(CCO)=O)=NN3CC)=CN=C2N)C
Synonyms :
AZD-8835
MDL No. :MFCD28902194

Safety of AZD-8835

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of AZD-8835

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • p110γ

    PI3Kγ, IC50:90 nM

  • p110β

    PI3Kβ, IC50:431 nM

  • p110α

    PI3Kα, IC50:6.2 nM

  • p110δ

    PI3Kδ, IC50:5.7 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
BmE cells 10 µM 72 hours Evaluate the cytotoxicity of AZD8835 on BmE cells, showing a cell viability of 83%. PMC6480691
BmE cells 10 µM 72 hours Evaluate the inhibitory effect of AZD8835 on BmNPV, showing accumulated virus DNA of 42%. PMC6480691
OVCAR-8 21.14-53.60 μM 48 hours AZD8835 inhibited BRCA1/BRCA2 mRNA expression and p-ERK protein expression. PMC7063971
PEO1 100 nM 24 h and 48 h Inhibits the PI3K/AKT pathway, reduces cell proliferation and induces cell death PMC9495868
HAC-2 4.64-9.41 μM 48 hours AZD8835 inhibited Akt phosphorylation and suppressed the expression of Akt downstream effectors 4E-BP1 and p70S6 kinase. PMC7063971
A2780CP70 4.64-9.41 μM 48 hours AZD8835 inhibited Akt phosphorylation and suppressed the expression of Akt downstream effectors 4E-BP1 and p70S6 kinase. PMC7063971
A2780 4.64-9.41 μM 48 hours AZD8835 inhibited Akt phosphorylation and suppressed the expression of Akt downstream effectors 4E-BP1 and p70S6 kinase. PMC7063971
MCF10A-PI3KαH1047R 250 nM 24 hours MAP3K1 knock-down in MCF10A-PI3KαH1047R made cells less sensitive to AZD8835-mediated pathway inhibition, as assessed by pPRAS40 signal. PMC5940413
T47D 250 nM 24 hours MAP3K1 knock-down in T47D made cells less sensitive to AZD8835-mediated pathway inhibition, as assessed by pPRAS40 signal. PMC5940413
MCF7 250 nM 24 hours MAP3K1 deficiency led to reduced inhibition of the pathway by AZD8835 and AZD5363 with a more pronounced effect on AZD5363 activity, indicated by maintained pP70S6K, pPRAS40 and pS6 ribosomal protein (RP) readouts in CR1.4 and CR2.5 compared with parent cells. PMC5940413
A204 cells 5 μM 72 hours Evaluate the effect of AZD8835 on A204 cell viability, results showed AZD8835 reduced cell viability PMC9104989
SJCRH30 cells 5 μM 72 hours Evaluate the effect of AZD8835 on SJCRH30 cell viability, results showed AZD8835 reduced cell viability PMC9104989
RD cells 5 μM 72 hours Evaluate the effect of AZD8835 on RD cell viability, results showed AZD8835 reduced cell viability PMC9104989
T-ALL cell lines 0.5 μM To evaluate the effect of AZD8835 on the proliferation of T-ALL cell lines, showing varying degrees of sensitivity to AZD8835. PMC5008349

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice Ovarian cancer xenograft model Oral 50 or 100 mg/kg Once daily, 2 days on: 5 days off for 21 days AZD8835 significantly inhibited tumor formation. PMC7063971
Mice CT-26, MC-38 and 4T1 tumor models Oral 50 mg/kg 2 days on/5 days off for 4 cycles AZD8835 significantly inhibited tumor growth by suppressing PI3Kα/δ signaling, enhanced CD8+ T-cell activation and memory function, and reduced immunosuppression by T-regs cells. PMC6307194
Silkworm larvae BmNPV infection model Oral 125 µg/g Only once Evaluate the inhibitory effect of AZD8835 on BmNPV in silkworm larvae, showing viral DNA content of 48% and mortality reduced to 12%. PMC6480691
Nude mice (nu/nu:Alpk) BT474C breast xenograft model Oral gavage 3, 6, 12.5, 25 or 50 mg/kg Single dose, imaging performed 2 hours post-dose To evaluate the minimally effective dose of AZD8835, a selective inhibitor of PI3Kα and PI3Kδ, and validate its potential as a pharmacodynamic biomarker using 18F-FDG PET imaging. Results showed that AZD8835 significantly reduced tumor 18F-FDG uptake at doses of 12.5, 25, and 50 mg/kg, with no significant reduction at 3 and 6 mg/kg. PMC5555689

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.30mL

4.26mL

2.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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