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Chemical Structure| 1191951-57-1 Chemical Structure| 1191951-57-1

Structure of PHT-427
CAS No.: 1191951-57-1

Chemical Structure| 1191951-57-1

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PHT-427 is dual inhibitor of Akt and PDPK1 with Ki of 2.7 μM and 5.2 μM, respectively, targeting PH domains of Akt and PDPK1.

Synonyms: Akt Inhibitor XIV; CS-0223

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Product Details of PHT-427

CAS No. :1191951-57-1
Formula : C20H31N3O2S2
M.W : 409.61
SMILES Code : O=S(C1=CC=C(CCCCCCCCCCCC)C=C1)(NC2=NN=CS2)=O
Synonyms :
Akt Inhibitor XIV; CS-0223
MDL No. :MFCD18384970
InChI Key :BYWWNRBKPCPJMG-UHFFFAOYSA-N
Pubchem ID :44240850

Safety of PHT-427

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H320-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of PHT-427

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • Akt

    Akt, Ki:2.7 μM

  • PDK1

    PDK1, Ki:5.2 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
BxPC-3 pancreatic cancer cells 10 µM 12-16 hours inhibition of Akt and PDKP1 signaling and their downstream targets PMC2837366
MiaPaCa-2 pancreatic cancer cells 10 µM 12-16 hours no significant inhibition of Akt and PDKP1 signaling PMC2837366
HaCaT human keratinocytes 100 nM 24 hours To investigate the effect of rapamycin on Akt signaling and test whether PHT-427 could block these effects. Results showed that rapamycin increased Akt (S473) phosphorylation, and PHT-427 significantly reduced rapamycin-induced Akt (S473) phosphorylation. PMC4777684
FaDu cells 0.5, 0.75, 1 mg/mL 24 or 48 hours To evaluate the effect of PHT-427-loaded nanoparticles on the proliferation and apoptosis of FaDu cells. Results showed that PHT-427 significantly enhanced its antiproliferative and proapoptotic activity by inactivating the PI3K/AKT/PDK1 pathway, inducing apoptosis. PMC8401941
Panc-1 pancreatic cancer cells 1, 5, 10 µM 4 hours inhibition of subcellular localization of Akt and PDKP1 PMC2837366

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Xenograft model IntratumOral injection 0.5 mg/ml and 1 mg/ml Once a week for four weeks To evaluate the anticancer efficacy of PHT-427 in head and neck squamous cell carcinoma, results showed that PHT-427 encapsulation increased drug efficacy and safety, as demonstrated by decreased tumor volume, reduced PI3K/AKT/PDK1 pathway expression, and improved antitumor activity and necrosis induction. PMC11727052
Mice immunodeficient mice Oral 125-250 mg/kg twice a day for 10 days inhibited the growth of human tumor xenografts with up to 80% inhibition in the most sensitive tumors PMC2837366
SKH-1 hairless mice SSL-induced skin tumor model Topical administration 3.7 µmol/back Three times a week for 10 weeks To investigate the inhibitory effect of PHT-427 combined with rapamycin on SSL-induced skin tumors. Results showed that the combination of PHT-427 and rapamycin significantly reduced tumor multiplicity. PMC4777684
Mice MiaPaCa-2 pancreatic cancer model Intraperitoneal injection SE-PLGA-427: 14 mg/kg, DE-PLGA-427: 19 mg/kg Once per week for four weeks To evaluate the therapeutic effect of PHT-427 in a pancreatic cancer model, the results showed that both SE-PLGA-427 and DE-PLGA-427 significantly reduced tumor volume and eliminated primary pancreatic tumors in 68% of the mice. PMC4983222

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.41mL

4.88mL

2.44mL

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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