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Chemical Structure| 1047644-62-1 Chemical Structure| 1047644-62-1

Structure of Afuresertib
CAS No.: 1047644-62-1

Chemical Structure| 1047644-62-1

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Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive, and potent pan-Akt kinase inhibitor with Kis of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively.

Synonyms: GSK2110183; LAE002

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Product Details of Afuresertib

CAS No. :1047644-62-1
Formula : C18H17Cl2FN4OS
M.W : 427.32
SMILES Code : O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN
Synonyms :
GSK2110183; LAE002
MDL No. :MFCD26961098
InChI Key :AFJRDFWMXUECEW-LBPRGKRZSA-N
Pubchem ID :46843057

Safety of Afuresertib

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

Related Pathways of Afuresertib

PI3K-AKT
Hedgehog

Isoform Comparison

Biological Activity

Target
  • Akt3

    Akt3, Ki:2.6 nM

  • Akt1

    Akt1, Ki:0.08 nM

  • Akt2

    Akt2, Ki:2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
K562 –FLT3ITD/WT cells 25 μM 5 days To investigate the effect of Afuresertib on CD52 expression, results showed that Afuresertib did not affect CD52 expression. PMC8149417
ML-2 cells 10 µM 24 hours Afuresertib enhanced the curcumin-induced cell cycle arrest and apoptosis in ML-2 cells. PMC7877002
OCI-AML5 cells 10 µM 24 hours Afuresertib enhanced the curcumin-induced cell cycle arrest and apoptosis in OCI-AML5 cells. PMC7877002
HEK293T cells 600 nM 0, 30, 45, 60 and 120 minutes Afuresertib inhibited phosphorylation of the AKT targets p-mTOR(S2448) and p-GSK3β(S9) without inhibiting p-AKT(S473) and inhibited the nonsense-mediated mRNA decay (NMD) of ATF3, GADD45A, and GADD45B mRNAs. PMC9357146
M#31 cells 10 µM 24 hours Investigated the sensitivity of M#31 cells to Afuresertib, showing that Afuresertib significantly enhanced cisplatin-induced cell death. PMC10721616
M#54 cells 10 µM 24 hours Investigated the effect of Afuresertib on M#54 cells, showing that Afuresertib did not significantly enhance cisplatin-induced cell death. PMC10721616
COS-7 cells 500 nM 6 hours Afuresertib effectively blocked the stimulatory effect of insulin on OAT1 transport activity. PMC10695010

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice subcutaneous and systemic Waldenström's models intraperitoneal injection 200 mg/kg/d Once daily for 14 days To evaluate the anti-tumor activity of R191 in Waldenstr?m's models, results showed that R191 significantly delayed tumor growth and prolonged survival of mice PMC6295253
NOD/SCID mice AML xenograft model oral 100 mg/kg Daily for 15 days Afuresertib in combination with curcumin significantly suppressed the engraftment, proliferation, and survival of AML cells. PMC7877002

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02177682 Neoplasms, Haematologic PHASE1 TERMINATED 2019-08-14 Novartis Investigative Site, A... More >>ichi, 467-8602, Japan|Novartis Investigative Site, Fukuoka, 811-1395, Japan|Novartis Investigative Site, Miyagi, 980-8574, Japan|Novartis Investigative Site, Niigata, 951-8566, Japan|Novartis Investigative Site, Tokyo, 104-0045, Japan Less <<
NCT01395004 Langerhans Cell Histiocytosis PHASE2 COMPLETED 2025-11-13 Johns Hopkins Hospital, Baltim... More >>ore, Maryland, 21287, United States|Dana Farber Cancer Institute, Boston, Massachusetts, 02115, United States|Memorial Sloan Kettering Cancer Center, New York, New York, 10065, United States|Staten Island University Hospital, Staten Island, New York, 10305, United States|Baylor College of Medicine, Houston, Texas, 77030, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.34mL

0.47mL

0.23mL

11.70mL

2.34mL

1.17mL

23.40mL

4.68mL

2.34mL

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
 

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