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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 dermal microvascular endothelial cells (HDMEC) 20 µM 16 hours Inhibited VEGF-A-driven Akt and downstream signaling pathways Cancer Res. 2008 Nov 15;68(22):9551-7.
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 Cancer Res. 2008 Nov 15;68(22):9551-7.
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 J Cell Biochem. 2017 Aug;118(8):2241-2249.
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. Br J Cancer. 2009 Mar 24;100(6):932-40.
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. Br J Cancer. 2009 Mar 24;100(6):932-40.
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. Br J Cancer. 2009 Mar 24;100(6):932-40.
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. Br J Cancer. 2009 Mar 24;100(6):932-40.
Human umbilical vascular endothelial cells (HUVEC) 10 µM 6 hours Induced endothelial cell apoptosis Cancer Res. 2008 Nov 15;68(22):9551-7.
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. Cancer Biol Ther. 2015;16(7):1047-55.
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. Cancer Biol Ther. 2015;16(7):1047-55.
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. Cancer Biol Ther. 2015;16(7):1047-55.
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. Br J Cancer. 2009 Mar 24;100(6):932-40.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NMRI Foxn1nu mice HROG05 xenograft model Local administration 1 mg/kg 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. Cancer Biol Ther. 2015;16(7):1047-55.
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%. Br J Cancer. 2009 Mar 24;100(6):932-40.
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 Cancer Res. 2008 Nov 15;68(22):9551-7.
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. Oncogene. 2011 May 26;30(21):2443-50

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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