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Chemical Structure| 914913-88-5 Chemical Structure| 914913-88-5

Structure of Palomid 529
CAS No.: 914913-88-5

Chemical Structure| 914913-88-5

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Palomid 529 is a novel dual mTORC1/2 inhibitor.

Synonyms: P529; RES-529; SG 00529

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Product Details of Palomid 529

CAS No. :914913-88-5
Formula : C24H22O6
M.W : 406.43
SMILES Code : O=C1C2=CC(C(O)C)=CC=C2C3=C(O1)C=C(OCC4=CC=C(OC)C=C4)C(OC)=C3
Synonyms :
P529; RES-529; SG 00529
MDL No. :MFCD18633224
InChI Key :YEAHTLOYHVWAKW-UHFFFAOYSA-N
Pubchem ID :11998575

Safety of Palomid 529

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P261-P302+P352-P305+P351+P338

Related Pathways of Palomid 529

PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • mTORC1

In Vitro:

Cell Line
Concentration Treated Time Description References
Human umbilical vascular endothelial cells (HUVEC) 10 μM 6 hours Induced endothelial cell apoptosis PMC2727940
Human dermal microvascular endothelial cells (HDMEC) 20 μM 16 hours Inhibited VEGF-A-driven Akt and downstream signaling pathways PMC2727940
C6V10 glioma cells 20 μM 2 or 24 hours Inhibited IGF-I-driven Akt and downstream signaling pathways, and inhibited mTOR association with rictor and raptor PMC2727940
Human lung fibroblasts 10–20 μM 24 hours P529 dose-dependently inhibited TGF-β-induced phosphorylation of S6K1 and 4E-BP1, with maximal inhibition occurring between 10–20 μM PMC5568785
PC-3 cells 2, 5, 7, 10 μM 48 hours Evaluate the growth inhibitory effect of P529 on PC-3 cells. Results showed that P529 has a concentration-dependent growth inhibitory effect on PC-3 cells, with a GI50 of 5-7 μM. PMC2661786
Leukemia and non-small cell lung cancer 2-34 μM (GI50) 48 hours Evaluate the growth inhibitory effect of P529 on various tumor cell lines. Results showed that P529 has broad-spectrum growth inhibitory effects on multiple tumor cell lines. PMC2661786
HROG10 7.5 μM 72 and 144 hours In HROG10 cells, the combination of ADI and Palomid 529 reduced cell numbers by 70% after 144 hours. PMC4623118
HROG05 7.5 μM 72 and 144 hours In HROG05 cells, the combination of ADI and Palomid 529 reduced cell numbers by 70% after 144 hours. PMC4623118
HROG02 7.5 μM 72 and 144 hours In HROG02 cells, the combination of ADI and Palomid 529 reduced cell numbers by 50% after 72 hours and 70% after 144 hours. PMC4623118
HUVECs 500 nM 96 hours Evaluate the growth inhibitory effect of P529 on HUVECs. Results showed that P529 significantly inhibited VEGF-stimulated endothelial cell proliferation. PMC2661786
Melanoma, colon and ovarian cancers 6-24 μM (GI50) 48 hours Evaluate the growth inhibitory effect of P529 on various tumor cell lines. Results showed that P530 has broad-spectrum growth inhibitory effects on multiple tumor cell lines.
CNS, renal, breast, and prostate cancer 2-19 μM (GI50) 48 hours Evaluate the growth inhibitory effect of P529 on various tumor cell lines. Results showed that P531 has broad-spectrum growth inhibitory effects on multiple tumor cell lines.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NMRI Foxn1nu mice HROG05 xenograft model Local administration 1 mg/kg bw Twice a week for a total of 6 injections Palomid 529 accelerated tumor growth, and the experiment had to be stopped at day 17 due to excessive tumor burden. PMC4623118
Male athymic nude mice PC-3 tumor model Subcutaneous injection 20 mg/kg Every 3 days for 4 weeks Evaluate the antitumor effect of P529 alone or in combination with radiotherapy on PC-3 tumor growth. Results showed that P529 alone reduced tumor volume by 42.9%, and in combination with radiotherapy reduced tumor volume by 77.4%. PMC2661786
Nude mice (nu/nu) C6V10 glioma model Intraperitoneal injection (i.p.) 200 mg/kg/2 days Every 2 days for 21 days Inhibited C6V10 glioma tumor growth, reduced tumor vascular density and glomeruloid vessel structures PMC2727940
NOD.SCID/NCR mice Brca1tr/tr MEFs-induced tumor model Oral 40mg/kg Once daily for 18 days To investigate the inhibitory effect of Palomid 529 on Brca1-deficient tumor growth, results showed that P529 significantly suppressed tumor growth and reduced tumor size. PMC3107712

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01033721 Age-Related Macular Degenerati... More >>on Less << PHASE1 COMPLETED 2025-12-11 Ophthalmic Consultants of Bost... More >>on, Boston, Massachusetts, 02114, United States Less <<
NCT01271270 Age-Related Macular Degenerati... More >>on Less << PHASE1 COMPLETED 2012-09-20 National Institutes of Health ... More >>Clinical Center, 9000 Rockville Pike, Bethesda, Maryland, 20892, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.46mL

0.49mL

0.25mL

12.30mL

2.46mL

1.23mL

24.60mL

4.92mL

2.46mL

References

 

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