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Chemical Structure| 2289691-01-4 Chemical Structure| 2289691-01-4

Structure of MYCi975
CAS No.: 2289691-01-4

Chemical Structure| 2289691-01-4

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MYCi975 improved analog of MYCi361 which is a MYC inhibitor. It showed better tolerability compared with MYCi361.

Synonyms: NUCC-0200975

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Product Details of MYCi975

CAS No. :2289691-01-4
Formula : C25H16Cl2F6N2O2
M.W : 561.30
SMILES Code : OC1=C(C2=CC(C(F)(F)F)=NN2C)C=CC(OCC3=CC=C(Cl)C=C3)=C1C4=CC=C(Cl)C(C(F)(F)F)=C4
Synonyms :
NUCC-0200975
MDL No. :MFCD32263413
InChI Key :VSDFDVBYONIJLD-UHFFFAOYSA-N
Pubchem ID :139600320

Safety of MYCi975

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of MYCi975

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
P493-6 cells 6 μM 24 hours To assess the effect of MYCi975 on MYC-dependent gene expression, results showed that MYCi975 significantly suppressed the expression of MYC target genes. Cancer Cell. 2019 Nov 11;36(5):483-497.e15.
PC3 cells 6 μM 1 hour To assess the effect of MYCi975 on MYC/MAX interaction, results showed that MYCi975 significantly disrupted the formation of MYC/MAX complex. Cancer Cell. 2019 Nov 11;36(5):483-497.e15.
HN12 cells 5 μM 48 hours To evaluate the effect of MYCi975 on cellular glutamine consumption, results showed that MYCi975 significantly inhibited glutamine consumption Cancer Res. 2024 Oct 1;84(19):3223-3234.
HN6 cells 5 μM 48 hours To evaluate the effect of MYCi975 on cellular glutamine consumption, results showed that MYCi975 significantly inhibited glutamine consumption Cancer Res. 2024 Oct 1;84(19):3223-3234.
MCF7 breast cancer cells 10 μM 48 hours MYCi975 treatment reduced FOXA1 occupancy at co-occurring ERα binding sites. Sci Adv. 2022 Apr 29;8(17):eabh3635.
P493-6 lymphoma cells 6 μM 24 hours MYCi975 treatment affected gene expression related to DNA metabolic process, DNA replication, and cell cycle pathways. Sci Adv. 2022 Apr 29;8(17):eabh3635.
PC3 prostate cancer cells 8 μM 24 hours MYCi975 treatment affected gene expression related to DNA metabolic process, DNA replication, and cell cycle pathways. Sci Adv. 2022 Apr 29;8(17):eabh3635.
22Rv1 prostate cancer cells 10 μM 1, 4, 8, 24, 48 hours Evaluated the kinetics of MYC protein down-regulation, MYCi975 induced MYC protein down-regulation in a time-dependent manner, achieving approximately >90% decrease in MYC protein levels by 48 hours. Sci Adv. 2022 Apr 29;8(17):eabh3635.
H929 cells 5 μM 48 hours Evaluate the effect of MYCi975 on H929 cells, showing MYCi975 enhanced T cell-mediated killing of H929 cells Clin Cancer Res. 2024 Jul 15;30(14):3023-3035.
Primary MM cells 1 μM 48 hours Evaluate the sensitivity of primary MM cells to MYCi975, showing 89% of samples were sensitive to MYCi975 with MYC protein degradation Clin Cancer Res. 2024 Jul 15;30(14):3023-3035.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MycCaP allograft model I.p. 100 mg/kg/day Once daily for 14 days To assess the inhibitory effect of MYCi975 on tumor growth, results showed that MYCi975 significantly inhibited tumor growth and increased tumor immune cell infiltration. Cancer Cell. 2019 Nov 11;36(5):483-497.e15.
Nude mice 22Rv1 xenograft model Oral 100 mg/kg BID 5 days a week for 3 weeks MYCi975 (100 mg/kg BID) led to a significant inhibition of tumor growth without any adverse effect on mouse body weight. Sci Adv. 2022 Apr 29;8(17):eabh3635.
NSG mice Orthotopic buccal mucosal tumor model Intraperitoneal injection 100 mg/kg Once daily for 15 days To evaluate the antitumor efficacy of MYCi975 alone or in combination with CB-839, results showed that the combination therapy significantly suppressed tumor growth and lymph node metastasis Cancer Res. 2024 Oct 1;84(19):3223-3234.
NOD/SCID mice HNSCC PDX model Intraperitoneal injection 100 mg/kg Every 2 days for 6 weeks Investigate the effect of MYCi975 on HNSCC PDX model, including inhibition of tumor growth and overcoming cisplatin resistance. Theranostics. 2024 Jan 1;14(2):622-639
BALB/c-nude female mice Cell line-derived xenograft model Subcutaneous injection 100 mg/kg Every 2 days for 4 weeks MYCi975 inhibited HNSCC growth and promoted CD8+ T cell infiltration. Oncoimmunology. 2022 Sep 30;11(1):2130583

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.91mL

1.78mL

0.89mL

17.82mL

3.56mL

1.78mL

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