[CAS NO. 2289690-31-7] MYCi361
PRODUCTS SPECIFICATIONS [2289690-31-7]
DESCRIPTION [2289690-31-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 594.86 |
| Molecular Formula | C26H16ClF9N2O2 |
| 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 |
1 Publications Citing Use of MCE
Summary
MYCi361 (NUCC-0196361) is a MYC inhibitor with the K d 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 IC 50 values [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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: | IC 50 s 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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 (C max ) of 27,200 ng/mL (46 μM) i.p. and 13,867 ng/mL (23 μM) p.o.. |
Appearance
Solid
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
DMSO : 100 mg/mL ( 168.11 mM ; Need ultrasonic)
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 |
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1.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.50 mM); Clear solution