PRI-724


Catalog No. size PriceQuantity
M6921-2 2mg solid $96
M6921-10 10mg solid $411

Description

Cas:1422253-38-0

Product Information:

PRI-724, also known as C-82 prodrug/ICG-001 analog, is a potent, specific inhibitor of the canonical Wnt signaling pathway in cancer stem cells with potential antineoplastic activity. Wnt signaling pathway inhibitor PRI-724 specifically inhibits the recruiting of beta-catenin with its coactivator CBP (the binding protein of the cAMP response element-binding protein CREB); together with other transcription factors beta-catenin/CBP binds to WRE (Wnt-responsive element) and activates transcription of a wide range of target genes of Wnt/beta-catenin signaling. Note: Chemical structures of ICG-001 and PRR-724 look very close, but they are not the same molecule. Many vendors confused them.

 

Chemical Formula: C33H35N6O7P

 

Exact Mass: 658.2305

 

Molecular Weight: 658.65

 

Elemental Analysis: C, 60.18; H, 5.36; N, 12.76; O, 17.00; P, 4.70

 

Related CAS #: 

1422253-38-0 (PRI-724)   

1198780-38-9   

847591-62-2 (deleted)   

780757-88-2 (ICG001)  

 

Synonym:

 

C-82 prodrug

ICG-001 analog

 

Chemical Name:

(6S,9S,9aS)-Hexahydro-2,9-dimethyl-4,7-dioxo-N-(phenylmethyl)-6-[[4-(phosphonooxy)phenyl]methyl]-8-(8-quinolinylmethyl)-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide

 

InChi Key:

VHOZWHQPEJGPCC-AZXNYEMZSA-N

 

InChi Code:

InChI=1S/C33H35N6O7P/c1-22-31-38(29(40)21-36(2)39(31)33(42)35-19-24-8-4-3-5-9-24)28(18-23-13-15-27(16-14-23)46-47(43,44)45)32(41)37(22)20-26-11-6-10-25-12-7-17-34-30(25)26/h3-17,22,28,31H,18-21H2,1-2H3,(H,35,42)(H2,43,44,45)/t22-,28-,31-/m0/s1

 

Smiles Code:

O=C(N([C@]([C@H](C)N1CC2=C3N=CC=CC3=CC=C2)([H])N4[C@@H](CC5=CC=C(OP(O)(O)=O)C=C5)C1=O)N(C)CC4=O)NCC6=CC=CC=C6

 

 

Technical Data:

 

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

 

In Vitro:

PRI-724 is phosphorylated-C-82 and is rapidly hydrolyzed to its active form C-82 in vivo. PRI-724 treatment reduces the fibrosis induced by CCl4 or BDL. C-82, an active form of PRI-724, inhibits the activation of isolated primary mouse quiescent hepatic stellate cells (HSCs) and promotes cell death in culture-activated HSCs.

 

 

References:

 

  1. Okazaki H, Sato S, Koyama K, Morizumi S, Abe S, Azuma M, Chen Y, Goto H, Aono Y, Ogawa H, Kagawa K, Nishimura H, Kawano H, Toyoda Y, Uehara H, Kouji H, Nishioka Y. The novel inhibitor PRI-724 for Wnt/β-catenin/CBP signaling ameliorates bleomycin-induced pulmonary fibrosis in mice. Exp Lung Res. 2019 Jul 12:1-12. doi: 10.1080/01902148.2019.1638466. [Epub ahead of print] PubMed PMID: 31298961.

 

  1. Rao P, Pang M, Qiao X, Yu H, Wang H, Yang Y, Ren X, Hu M, Chen T, Cao Q, Wang Y, Khushi M, Zhang G, Wang YM, Heok P'ng C, Nankivell B, Lee VW, Alexander SI, Zheng G, Harris DC. Promotion of β-catenin/Foxo1 signaling ameliorates renal interstitial fibrosis. Lab Invest. 2019 Jun 26. doi: 10.1038/s41374-019-0276-z. [Epub ahead of print] PubMed PMID: 31243340.

 

  1. Osawa Y, Kojika E, Nishikawa K, Kimura M, Osakaya S, Miyauchi H, Kanto T, Kawakami Y, Kimura K. Programmed cell death ligand 1 (PD-L1) blockade attenuates metastatic colon cancer growth in cAMP-response element-binding protein (CREB)-binding protein (CBP)/β-catenin inhibitor-treated livers. Oncotarget. 2019 Apr 30;10(32):3013-3026. doi: 10.18632/oncotarget.26892. eCollection 2019 Apr 30. PubMed PMID: 31105882; PubMed Central PMCID: PMC6508964.

 

  1. Kleszcz R, Szymańska A, Krajka-Kuźniak V, Baer-Dubowska W, Paluszczak J. Inhibition of CBP/β-catenin and porcupine attenuates Wnt signaling and induces apoptosis in head and neck carcinoma cells. Cell Oncol (Dordr). 2019 Aug;42(4):505-520. doi: 10.1007/s13402-019-00440-4. Epub 2019 May 14. PubMed PMID: 31089983.

 

  1. Bocchicchio S, Tesone M, Irusta G. Convergence of Wnt and Notch signaling controls ovarian cancer cell survival. J Cell Physiol. 2019 May 13. doi: 10.1002/jcp.28775. [Epub ahead of print] PubMed PMID: 31087357.

 

Products are for research use only. Not for human use.

 

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