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Chemical Structure| 873652-48-3 Chemical Structure| 873652-48-3

Structure of GDC-0152
CAS No.: 873652-48-3

Chemical Structure| 873652-48-3

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GDC-0152 is a potent inhibitor of IAPs and binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2 with K (i) values of 28, 14, 17, and 43 nM, respectively.

Synonyms: GDC-0152

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Product Details of GDC-0152

CAS No. :873652-48-3
Formula : C25H34N6O3S
M.W : 498.64
SMILES Code : O=C(N1[C@H](C(NC2=C(C3=CC=CC=C3)N=NS2)=O)CCC1)[C@H](C4CCCCC4)NC([C@H](C)NC)=O
Synonyms :
GDC-0152
MDL No. :MFCD26142660
InChI Key :WZRFLSDVFPIXOV-LRQRDZAKSA-N
Pubchem ID :46940575

Safety of GDC-0152

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

Isoform Comparison

Biological Activity

Target
  • cIAP

    cIAP1-BIR3, Ki:17 nM

    cIAP2-BIR3, Ki:43 nM

  • XIAP

    XIAP-BIR3, Ki:28 nM

    XIAP-BIR2, Ki:112 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HIV-infected resting memory CD4+ T cells (HIV-T CM) 10 nM 24 hours Induced cell death in HIV-T CM without increasing virus production PMC6250054
C8B4 cells 1 µM 72 hours GDC-0152 promoted the anti-tumoral function of C8B4 cells via caspase-3 pro-inflammatory cleavage and NF-κB activation, and inhibited the growth of tumoroids. PMC11402972
Human glioblastoma-derived CD45+ cells 1 µM 72 hours GDC-0152 treatment altered the morphology of CD45+ cells, increasing their area and affecting cytokine secretion, indicating functional changes. PMC11402972

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MDA-MB-231 breast cancer xenograft model Oral 10, 50, 100 mg/kg once weekly or daily for three weeks Assessed anti-tumor activity of GDC-0152, results showed GDC-0152 significantly inhibited tumor growth PMC3366583

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00977067 Solid Cancers PHASE1 TERMINATED 2025-11-09 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.03mL

2.01mL

1.00mL

20.05mL

4.01mL

2.01mL

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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