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Chemical Structure| 1143532-39-1 Chemical Structure| 1143532-39-1

Structure of Capivasertib
CAS No.: 1143532-39-1

Chemical Structure| 1143532-39-1

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Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 values of 3 nM, 7 nM, and 7 nM for Akt1, Akt2, and Akt3, respectively.

Synonyms: AZD5363

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Product Details of Capivasertib

CAS No. :1143532-39-1
Formula : C21H25ClN6O2
M.W : 428.92
SMILES Code : O=C(C1(N)CCN(C2=C3C(NC=C3)=NC=N2)CC1)N[C@H](C4=CC=C(Cl)C=C4)CCO
Synonyms :
AZD5363
MDL No. :MFCD22628785
InChI Key :JDUBGYFRJFOXQC-KRWDZBQOSA-N
Pubchem ID :25227436

Safety of Capivasertib

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

Related Pathways of Capivasertib

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • Akt3

    Akt3, IC50:8 nM

  • Akt1

    Akt1, IC50:3 nM

  • Akt2

    Akt2, IC50:8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
T47D 0.01 –10μM 72 h To evaluate the inhibitory effect of Capivasertib on T47D cells, results showed that T47D cells had an IC50 value of 2.1 μM and were more sensitive to Capivasertib than MCF-7 cells. Br J Cancer. 2024 Nov;131(9):1543-1554.
MCF-7 0.01 –10μM 72 h To evaluate the inhibitory effect of Capivasertib on MCF-7 cells, results showed that MCF-7 cells had an IC50 value of 7.5 μM and were less sensitive to Capivasertib than T47D cells. Br J Cancer. 2024 Nov;131(9):1543-1554.
Onc-negativeRAS/PI3K murine cell lines 10 μM 2 days To evaluate the effect of Capivasertib on cell proliferation and apoptosis. Results showed that Capivasertib significantly inhibited cell proliferation and induced apoptosis. Cancer Res. 2022 Apr 15;82(8):1589-1602.
MCF-7 500 nM 6 days To evaluate the growth inhibitory effect of Capivasertib in MCF-7 cells, the results showed that the triple combination (fulvestrant, CDK4/6i, and AKTi) significantly inhibited the growth of fulvestrant-resistant cells Nat Commun. 2021 Aug 25;12(1):5112.
T47D 200 nM 6 days To evaluate the growth inhibitory effect of Capivasertib in T47D cells, the results showed that the triple combination (fulvestrant, CDK4/6i, and AKTi) significantly inhibited the growth of fulvestrant-resistant cells Nat Commun. 2021 Aug 25;12(1):5112.
ZR-75-1 150 nM 6 days To evaluate the growth inhibitory effect of Capivasertib in ZR-75-1 cells, the results showed that the triple combination (fulvestrant, CDK4/6i, and AKTi) significantly inhibited the growth of fulvestrant-resistant cells Nat Commun. 2021 Aug 25;12(1):5112.
AN3-CA 1 µM 74 h To validate the combination activity of Capivasertib with AZD5991 in endometrial cancer cells, results showed induction of apoptosis in AN3-CA and MFE-296 cells. Cancer Discov. 2024 May 1;14(5):846-865.
MFE-296 1 µM 74 h To validate the combination activity of Capivasertib with AZD5991 in endometrial cancer cells, results showed induction of apoptosis in AN3-CA and MFE-296 cells. Cancer Discov. 2024 May 1;14(5):846-865.
HCC70 500 nM 4 days To evaluate the sensitivity of HCC70 cells to Capivasertib, the results showed that Capivasertib significantly inhibited cell proliferation. Oncogene. 2022 Nov;41(46):5046-5060.
EVSA-T 1 µM 4 days To evaluate the sensitivity of EVSA-T cells to Capivasertib, the results showed that Capivasertib significantly inhibited cell proliferation. Oncogene. 2022 Nov;41(46):5046-5060.
SNU-1196-GR 2 μM 72 h To evaluate the sensitivity of SNU-1196-GR cells to Capivasertib, results showed that Capivasertib reduced the IC50 value of GEM. Int J Biol Sci. 2023 May 21;19(9):2772-2786.
SSP-25-GR 2 μM 24 h To evaluate the effect of Capivasertib on hENT1 expression in SSP-25-GR cells, results showed that Capivasertib enhanced hENT1 expression. Int J Biol Sci. 2023 May 21;19(9):2772-2786.
MDA-MB-231 cells 0.1 μM 48 h To investigate the effect of Capivasertib on DOX-induced cell death in DNAJC12-overexpressing cells, results showed that Capivasertib significantly decreased cell viability in the DNAJC12-overexpressing group, approaching the level observed with DOX treatment alone in the negative control group. Redox Biol. 2024 Apr;70:103035.
MCF-7 cells 0.1 μM 48 h To investigate the effect of Capivasertib on DOX-induced cell death in DNAJC12-knockdown cells, results showed that Capivasertib significantly decreased cell viability in the negative control group, approaching the level observed with DOX treatment alone in the DNAJC12 knockdown group. Redox Biol. 2024 Apr;70:103035.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID mice MCF7 xenograft model Oral 150 mg/kg Twice daily for 28 days AZD5363 treatment significantly reduced (22%) mean tumor volume (MTV) of MCF7 parental tumors whereas it had no effect on MCF7 CR2.5 tumors, at day 18 of treatment. Oncotarget. 2018 Apr 20;9(30):21444-21458.
Mice TC mice Oral 100 mg/kg Daily for eight days, stopped for two days for recovery, and continued for two more days To evaluate the effect of Capivasertib alone or in combination with RMC-4550 on tumor burden. Results showed that Capivasertib alone was ineffective in vivo, but the combination with RMC-4550 significantly reduced tumor burden. Cancer Res. 2022 Apr 15;82(8):1589-1602.
Mice Breast cancer xenograft model Oral 100 mg/kg 5 days per week for 7 weeks To evaluate the anti-tumor effect of Capivasertib in a breast cancer xenograft model, the results showed that the triple combination (fulvestrant, CDK4/6i, and AKTi) significantly inhibited tumor growth and prevented tumor recurrence Nat Commun. 2021 Aug 25;12(1):5112.
Mice PTEN-deficient prostate cancer PDX model Intraperitoneal injection 2.5 mg/kg Daily, continuous treatment To evaluate whether the CX3CR1 inhibitor JMS-17-2 could sensitize PTEN-deficient prostate cancer to the AKT inhibitor Capivasertib. The results showed that JMS-17-2 significantly enhanced the inhibitory effect of Capivasertib on PDX growth. J Clin Invest. 2024 May 23;134(14):e175949
Mice NOMO-1 xenograft model Oral 10 mg/kg Twice daily for 28 days To evaluate the in vivo activity of Capivasertib with AZD5991 in the NOMO-1 xenograft model, results showed significant tumor growth inhibition. Cancer Discov. 2024 May 1;14(5):846-865.
Female nude mice HCC70 tumor xenograft model Oral 130 mg/kg Twice daily for 4 days To evaluate the anti-tumor activity of Capivasertib in combination with AZD5991 in the HCC70 tumor xenograft model, the results showed that the combination significantly inhibited tumor growth. Oncogene. 2022 Nov;41(46):5046-5060.
BALB/c nude mice SNU-1196-GR xenograft model Oral gavage 100 mg/kg Five times per week for 3 weeks To evaluate the effect of Capivasertib in combination with GEM on tumor growth in the SNU-1196-GR xenograft model, results showed that the combination treatment significantly inhibited tumor growth. Int J Biol Sci. 2023 May 21;19(9):2772-2786.
BALB/c nude mice MDA-MB-231 cell-derived xenograft model Intraperitoneal injection 50 mg/kg Every three days for a total of 5 injections To investigate the reversal effect of Capivasertib on DNAJC12-induced DOX resistance, results showed that the combination of Capivasertib and DOX significantly reduced tumor volume in the DNAJC12-overexpressing group, reversing DOX resistance. Redox Biol. 2024 Apr;70:103035.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01353781 Advanced Solid Malignancy|Adva... More >>nced Solid Tumor Less << PHASE1 COMPLETED 2025-07-14 Research Site, Chuo-ku, Japan
NCT06613516 Breast Cancer|Oestrogen Recept... More >>or Positive Breast Cancer Less << PHASE2 NOT_YET_RECRUITING 2027-11-01 Imperial College Healthcare Tr... More >>ust, London, United Kingdom Less <<
NCT02077569 Invasive Breast Cancer PHASE2 COMPLETED 2017-02-21 Royal Derby Hospital, Derby, D... More >>erbyshire, DE22 3DT, United Kingdom|Plymouth Hospitals NHS Trust, Derriford, Plymouth, Devon, PL6 8DH, United Kingdom|Royal Bournemouth Hospital, Bournemouth, Dorset, BH7 7DW, United Kingdom|Poole Hospital NHS Foundation Trust, Poole, Dorset, BH15 2JB, United Kingdom|Leicester Royal Infirmary, Leicester, Leicestershire, LE1 5WW, United Kingdom|Western General Hospital, Edinburgh, Lothian, EH4 2XU, United Kingdom|Royal Liverpool University Hospital, Liverpool, Merseyside, L7 8XP, United Kingdom|Kingsmill Hospital, Sutton-in-Ashfield, Nottinghamshire, NG17 4JL, United Kingdom|Sheffield Cancer Research Centre, Sheffield, South Yorkshire, S10 2SJ, United Kingdom|University Hospital Birmingahm, Birmingham, West Midlands, B15 2TT, United Kingdom|Leeds St James Institue of Oncology, Leeds, West Yorkshire, LS9 7TF, United Kingdom Less <<
NCT05008055 Relapsed or Refractory B-cell ... More >>Non-Hodgkin Lymphoma Less << PHASE2 COMPLETED 2024-10-25 Research Site, Duarte, Califor... More >>nia, 91010, United States|Research Site, Los Angeles, California, 90095, United States|Research Site, Houston, Texas, 77030, United States|Research Site, Victoria, British Columbia, V8R 6V5, Canada|Research Site, Aarhus N, DK8200, Denmark|Research Site, Poitiers, 86021, France|Research Site, Villejuif Cedex, 94805, France|Research Site, Busan, 49241, Korea, Republic of|Research Site, Seoul, 06351, Korea, Republic of|Research Site, Seoul, 3722, Korea, Republic of|Research Site, Badalona, 08003, Spain|Research Site, Barcelona, 8035, Spain|Research Site, Madrid, 28040, Spain|Research Site, Madrid, 28046, Spain|Research Site, Cambridge, CB2 0QQ, United Kingdom|Research Site, Manchester, M20 4BX, United Kingdom|Research Site, Sutton, SM2 5PT, United Kingdom Less <<
NCT04439123 Advanced Lymphoma|Advanced Mal... More >>ignant Solid Neoplasm|Hematopoietic and Lymphoid Cell Neoplasm|Refractory Lymphoma|Refractory Malignant Solid Neoplasm|Refractory Multiple Myeloma Less << PHASE2 ACTIVE_NOT_RECRUITING 2025-03-05 ECOG-ACRIN Cancer Research Gro... More >>up, Philadelphia, Pennsylvania, 19103, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.66mL

2.33mL

1.17mL

23.31mL

4.66mL

2.33mL

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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