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MYCi975

Chemical Structure : MYCi975

CAS No.: 2289691-01-4

MYCi975 (NUCC-0200975, MYCi 975)

Catalog No.: PC-73127Not For Human Use, Lab Use Only.

MYCi975 (NUCC-0200975) is a close analog of MYCi361 with improved therapeutic index, binds to MYC protein with KD of 2.5 uM, disrupts MYC/MAX complex formation.

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5 mg $188 In stock
10 mg $298 In stock
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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MYCi975 (NUCC-0200975) is a close analog of MYCi361 with improved therapeutic index, binds to MYC protein with KD of 2.5 uM, disrupts MYC/MAX complex formation.
MYCi975 (8 uM) enhances MYC degradation and phosphorylation on T58 in treated cells, also directly increases GSK3β-mediated MYC pT58 in the in vitro kinase assay at 6 uM.
MYCi975 inhibits MYC-dependent cancer cell viability and suppresses MYC transcriptional activity.
MYCi975 increases tolerability at significantly higher doses.
MYCi975 exhibits excellent pharmacokinetic profiles following p.o., i.p. or i.v. administration.
MYCi975 (100 mg/kg/day) inhibits tumor growth in MycCaP allografts with no changes in body weight.
MYCi975 synergized with Ara-C with no obvious impact in NSG mice bearing MV-411 AML xenografts.

Physicochemical Properties

M.Wt 561.31
Formula C25H16Cl2F6N2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4'-chloro-6-((4-chlorobenzyl)oxy)-3-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-5-yl)-3'-(trifluoromethyl)-[1,1'-biphenyl]-2-ol

References

1. Han H, et al. Cancer Cell. 2019 Nov 11;36(5):483-497.e15.

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