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Chemical Structure| 1009298-09-2 Chemical Structure| 1009298-09-2

Structure of AZD-8055
CAS No.: 1009298-09-2

Chemical Structure| 1009298-09-2

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AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM, inhibiting both mTORC1 and mTORC2.

Synonyms: CCG-168

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Product Details of AZD-8055

CAS No. :1009298-09-2
Formula : C25H31N5O4
M.W : 465.54
SMILES Code : OCC1=CC(C2=NC3=NC(N4[C@@H](C)COCC4)=NC(N5[C@@H](C)COCC5)=C3C=C2)=CC=C1OC
Synonyms :
CCG-168
MDL No. :MFCD16660191
InChI Key :KVLFRAWTRWDEDF-IRXDYDNUSA-N
Pubchem ID :25262965

Safety of AZD-8055

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

Related Pathways of AZD-8055

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • mTOR

    mTOR (full length), IC50:0.8 nM

    mTOR (truncated), IC50:0.13 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
KRAS mutant colorectal cancer cells 500 nM 16 hours AZD8055 effectively suppressed MCL-1 expression in KRAS mutant cells but not in KRAS/BRAF wild-type cells PMC3973435
PANC-1 cells 10 nM, 100 nM, 500 nM 48 hours AZD-8055 combined with radiation significantly inhibited cell growth and induced apoptosis PMC3726417
KRAS mutant HCT-116 cells 500 nM 72 hours AZD8055 combined with ABT-263 significantly induced apoptosis in KRAS mutant cells but had no significant effect in KRAS wild-type cells PMC3973435
Renca cells 50 ng/ml 72 hours To evaluate the inhibitory effect of AZD8055 on the growth of Renca cells, the results showed that AZD8055 significantly inhibited the growth of Renca cells. PMC3116937
KEP1.23 cells 25 nM 7 days To evaluate the effect of MYC overexpression on AZD-8055 sensitivity, results showed that MYC-overexpressing cells had reduced sensitivity to AZD-8055. PMC10465700
KEP2.E3 cells 25 nM 7 days To evaluate the effect of MYC overexpression on AZD-8055 sensitivity, results showed that MYC-overexpressing cells had reduced sensitivity to AZD-8055. PMC10465700
SUM52PE cells 200 nM 10 days To evaluate the effect of MYC overexpression on AZD-8055 sensitivity, results showed that MYC-overexpressing cells had reduced sensitivity to AZD-8055. PMC10465700
MDA-MB-468 cells 200 nM 10 days To evaluate the effect of MYC overexpression on AZD-8055 sensitivity, results showed that MYC-overexpressing cells had reduced sensitivity to AZD-8055. PMC10465700

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MYC/Trp53-/- liver cancer model Oral 75 mg/kg twice daily for 3 weeks To evaluate the therapeutic effect of AZD-8055 on liver cancer in Hpcal1-deficient mice, results showed that AZD-8055 significantly inhibited tumor growth PMC9691343
Mice Wild-type mice Intraperitoneal injection 5 mg/kg administered on days 0, 3, 6, and 9, monitored for 13 days AZD8055 significantly increased urine volume and sodium excretion but had no significant effect on potassium and chloride excretion, indicating that mTOR primarily influences sodium balance through regulation of ENaC function. PMC4382226
Mice KRAS mutant colorectal cancer xenograft model Oral 2.5 mg/kg Once daily for 21 days The combination of AZD8055 and ABT-263 significantly inhibited tumor growth in KRAS mutant models but had no significant effect in KRAS wild-type models PMC3973435
Nude mice PANC-1 xenograft model Oral 15 mg/kg Single injection, 6-hour duration AZD-8055 combined with fractionated radiation significantly enhanced the antitumor effect, with a significant reduction in tumor volume PMC3726417
Mice Metastatic renal cell carcinoma model Oral 5 mg/kg Single dose, lasting 6 or 24 hours To evaluate the anti-tumor effect of AZD8055 in combination with αCD40 antibody, the results showed that the combination treatment significantly reduced the number of tumor nodules in the liver and increased the infiltration and activation of CD8+ T cells and NK cells. PMC3116937
Mice ILC tumor model Oral 1.234 mg/kg Twice weekly for 2 weeks, then daily for an additional 10 days To evaluate the resistance effect of MYC overexpression on AZD-8055 treatment, results showed that MYC-overexpressing tumors had significantly reduced efficacy to AZD-8055 treatment. PMC10465700

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00999882 Cancer Advanc... More >>ed Hepatocellular Carcinoma Less << Phase 1 Completed - Hong Kong ... More >> Research Site Hong Kong, Hong Kong Korea, Republic of Research Site Seongnam, Gyeonggi-do, Korea, Republic of Research Site Seoul, Korea, Republic of Less <<
NCT01194193 Cancer Advanc... More >>ed Solid Tumours Lymphomas Less << Phase 1 Withdrawn(Amendment to study c... More >>ompound development programme) Less << - -
NCT00973076 Cancer Solid ... More >>Tumors Advanced Solid Malignancies Less << Phase 1 Completed - Japan ... More >> Research Site Tokyo, Japan Less <<
NCT01316809 Glioblastoma Multiforme ... More >> Anaplastic Astrocytoma Anaplastic Oligodendroglioma Malignant Glioma Brainstem Glioma Less << Phase 1 Completed - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less <<
NCT00731263 Solid Tumors Phase 1 Completed - United States, New York ... More >> Research Site New York, New York, United States, 10065 United States, Texas Research Site Houston, Texas, United States France Research Site Clichy, France United Kingdom Research Site Sutton, Surrey, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.21mL

10.74mL

2.15mL

1.07mL

21.48mL

4.30mL

2.15mL

References

 

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