| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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MYCi361 (NUCC0196361) is a novel and potent MYC inhibitor (Kd = 3.2 μM) with potential anticancer activity, it demonstrated a narrow therapeutic index. MYCi361 phosphorylated MYC within cells, shattered MYC/MAX dimers, and reduced MYC-stimulated transcription. Additionally, it increased the phosphorylation of MYC on threonine-58, which increased the degradation of MYC by proteasomes. MYCi361 has the ability to improve anti-PD1 immunotherapy and inhibit tumor growth.
| Targets |
MYC (Kd = 3.2 μM)
|
|---|---|
| ln Vitro |
MYCi361 inhibits MYC-driven gene expression, breaks down MYC/MAX dimers, and activates MYC inside of cells. MYCi361 increases MYC phosphorylation on threonine-58, which in turn increases MYC degradation by the proteasome.[1]
|
| ln Vivo |
MYCi361 upregulates PD-L1 on tumors, enhances tumor immune cell infiltration, inhibits in vivo tumor growth in mice, and makes tumors more susceptible to anti-PD1 immunotherapy.[1]
|
| Cell Assay |
The supernatants are obtained after treating MycCaP cells with 4 μM MYCi361 for a duration of 72 hours. To quantify high mobility group protein B1 (HMGB1) and secreted ATP, cell counts are carried out. After incubating cells with rabbit anti-Calreticulin for 60 minutes, they are subjected to an analysis by flow cytometry using Alexa Flour 488 anti-rabbit secondary antibody to detect the presence of surface Calreticulin.
|
| Animal Protocol |
6-8 week old FVB mice, prostate PDX model, NSG mice, C57BL/6 mice, CB17/Icr-Prkdcscid/IcrIcoCrl mice, CD-1 mice
55 mg/kg, 50 mg/kg IP, Oral gavage |
| References |
| Molecular Formula |
C26H16CLF9N2O2
|
|---|---|
| Molecular Weight |
594.8561
|
| Exact Mass |
594.075
|
| Elemental Analysis |
C, 52.50; H, 2.71; Cl, 5.96; F, 28.74; N, 4.71; O, 5.38
|
| CAS # |
2289690-31-7
|
| Related CAS # |
2289690-31-7;
|
| PubChem CID |
139600319
|
| Appearance |
White to off-white solid powder
|
| LogP |
7.9
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
12
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
40
|
| Complexity |
813
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
CKLCWLSEYDDTCN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C26H16ClF9N2O2/c1-38-19(11-21(37-38)26(34,35)36)18-6-7-20(40-12-13-2-4-17(27)5-3-13)22(23(18)39)14-8-15(24(28,29)30)10-16(9-14)25(31,32)33/h2-11,39H,12H2,1H3
|
| Chemical Name |
2-[3,5-bis(trifluoromethyl)phenyl]-3-[(4-chlorophenyl)methoxy]-6-[2-methyl-5-(trifluoromethyl)pyrazol-3-yl]phenol
|
| Synonyms |
NUCC-0196361; NUCC0196361; NUCC 0196361; MYC i361; MYCi361; MYC-i361
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~168.1 mM)
Ethanol: ~14 mg/mL (~23.5 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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