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Chemical Structure| 1207360-89-1 Chemical Structure| 1207360-89-1

Structure of GDC-0349
CAS No.: 1207360-89-1

Chemical Structure| 1207360-89-1

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GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, showing > 700-fold selectivity over PI3Kα and other 266 kinases.

Synonyms: RG-7603

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Product Details of GDC-0349

CAS No. :1207360-89-1
Formula : C24H32N6O3
M.W : 452.55
SMILES Code : O=C(NC1=CC=C(C2=NC(N3[C@@H](C)COCC3)=C4C(CN(C5COC5)CC4)=N2)C=C1)NCC
Synonyms :
RG-7603
MDL No. :MFCD22417087

Safety of GDC-0349

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Related Pathways of GDC-0349

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • mTOR

    mTOR, Ki:3.8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
A549 cells 5-500 nM 24-96 hours GDC-0349 inhibited A549 cell viability in a concentration- and time-dependent manner, significantly reducing colony formation and proliferation, inducing G1-S phase arrest, and inhibiting cell migration and invasion. PMC7644631
BEAS-2B epithelial cells and primary human lung epithelial cells 100 nM GDC-0349 did not induce viability reduction or apoptosis in BEAS-2B epithelial cells and primary human lung epithelial cells. PMC7644631
Primary human NSCLC cells (NSCLC-1/-2/-3) 100 nM GDC-0349 significantly reduced viability, proliferation, and migration of primary NSCLC cells. PMC7644631

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID mice A549 or NSCLC-1 xenograft model Oral 10 or 30 mg/kg Once daily for 21 days Oral administration of GDC-0349 significantly inhibited the growth of A549 and NSCLC-1 xenografts without causing significant toxicity. PMC7644631
Athymic mice MCF7-neo/Her2 tumor xenograft model Oral 10, 20, 30, 40, 50, 60, 70, 80 mg/kg Once daily To evaluate the dose-dependent antitumor efficacy of GDC-0349 in the MCF7-neo/Her2 tumor model, results showed tumor growth stasis (99% TGI) at the maximum tolerated dose. PMC4027466

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01356173 Non-Hodgkin's Lymphoma, Solid ... More >>Tumor Less << PHASE1 COMPLETED 2025-12-12 Scottsdale, Arizona, 85258, Un... More >>ited States|Toronto, Ontario, M5G 2M9, Canada Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.05mL

2.21mL

1.10mL

22.10mL

4.42mL

2.21mL

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

References

 

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