MYCi361

SKU: orb1220011

Description

MYCi361 is an inhibitor of MYC (binding to MYC with Kd of 3.2 μM). MYCi361 is a small-molecule MYC inhibitors that inhibits the viability of MYC-dependent cancer cells including prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2) with low-micromolar IC50 values.MYC inhibitor 361 (MYCi361), suppressed in vivo tumor growth in mice, increased tumor immune cell infiltration, upregulated PD-L1 on tumors, and sensitized tumors to anti-PD1 immunotherapy.

Key Properties

• CAS Number: 2289690-31-7
• MW: 594.86
• Purity: >98% (HPLC)
• Formula: C₂₆H₁₆ClF₉N₂O₂
• SMILES: Cn1nc(cc1-c1ccc(OCc2ccc(Cl)cc2)c(-c2cc(cc(c2)C(F)(F)F)C(F)(F)F)c1O)C(F)(F)F
• Target: c-Myc
• Solubility: DMSO:100 mg/mL (168.1 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  MYCi361 inhibits MYC-dependent tumor growth In vivo. MYCi361 treatment (100 mg/kg/day for 2 days; then 70 mg/kg/day for 9 days) induces tumor regression in FVB or NSG male mice. MYCi361 has moderate terminal elimination half-life of 44 and 20 h for intraperitoneal (i.p.) or oral (p.o.) dosing in mice, respectively. MYCi361 suppresses tumor growth in mice, increases tumor immune cell infiltration, upregulates PD-L1 on tumors, and sensitizes tumors to anti-PD1 immunotherapy. However, MYCi361 demonstrates a narrow therapeutic index. An improved analog, MYCi975 shows better tolerability. Animal model: FVB or NSG male mice of 6-8 weeks of age and 25 g bearing established MycCaP tumors. Dosage: 50 mg/kg and 70 mg/kg. Administration: Treatment i.p. initially at 50 mg/kg twice daily for 2 days, then 70 mg/kg/day for 9 days. Result: Induced tumor regression. Animal model: C57BL/6 mice. Dosage: 50 mg/kg (Pharmacokinetic analysis). Administration: Treated p.o. or i.p.; 24 hours. Result: Intraperitoneal (i.p.) or oral (p.o.) dosing in mice indicated plasma half-lives of 44 and 20 h, respectively, with maximum plasma concentrations (Cmax) of 27, 200 ng/mL (46 μM) i.p. and 13, 867 ng/mL (23 μM) p.o.
• In Vitro:
  MYCi361 inhibits the viability of MYC-dependent cancer cells including prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2) with low-micromolar IC50 values. Cell Proliferation Assay Cell line: The prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2). Concentration: 1.4-5.0 μM Incubation time: 5 days. Result: IC50s of 2.9, 1.4, 1.6, 2.6, 5.0, 2.1, and 4.9 μM for prostate cancer (MycCaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2), respectively.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NUCC-0196361

Quick Database Links

Gene Symbol

c-Myc