1. Apoptosis
  2. c-Myc
  3. MYCi361

MYCi361 (Synonyms: NUCC-0196361)

Cat. No.: HY-129600 Purity: 98.31%
Handling Instructions

MYCi361 (NUCC-0196361) is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 (NUCC-0196361) suppresses tumor growth and enhances anti-PD1 immunotherapy.

For research use only. We do not sell to patients.

MYCi361 Chemical Structure

MYCi361 Chemical Structure

CAS No. : 2289690-31-7

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Description

MYCi361 (NUCC-0196361) is a MYC inhibitor with the Kd of 3.2 μM for binding to MYC. MYCi361 (NUCC-0196361) suppresses tumor growth and enhances anti-PD1 immunotherapy[1].

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[1].

Cell Proliferation Assay[1]

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.
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[1].
MYCi361 has moderate terminal elimination half-life of 44 and 20 h for intraperitoneal (i.p.) or oral (p.o.) dosing in mice, respectively[1].
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[1].

Animal Model: FVB or NSG male mice of 6-8 weeks of age and 25 g bearing established MycCaP tumors[1]
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[1]
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..
Molecular Weight

594.86

Formula

C₂₆H₁₆ClF₉N₂O₂

CAS No.

2289690-31-7

SMILES

ClC1=CC=C(COC2=CC=C(C3=CC(C(F)(F)F)=NN3C)C(O)=C2C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (184.92 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6811 mL 8.4053 mL 16.8107 mL
5 mM 0.3362 mL 1.6811 mL 3.3621 mL
10 mM 0.1681 mL 0.8405 mL 1.6811 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: 98.31%

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Keywords:

MYCi361NUCC-0196361MYCi 361MYCi-361NUCC0196361NUCC 0196361c-MycMycInhibitorinhibitorinhibit

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