MYCi361 (Synonyms: NUCC-0196361) |
Catalog No.GC38589
One-Click Copy Product Info
|
MYCi361 is a kind of MYC inhibitor with a KD value for binding to MYC of 3.2μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2289690-31-7
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
MYCi361 is a kind of MYC inhibitor with a KD value for binding to MYC of 3.2μM [1]. MYCi361 can bind to MYC and disrupt MYC/MAX complex formation, while also decrease MYC protein stability, which lead to significant inhibition of MYC-dependent cancer-cell proliferation in vitro and inhibition of tumor growth in vivo [1]. MYCi361 showed excellent pharmacokinetic profiles, with long terminal half-lives, high peak plasma concentration, and tumor penetration [1].
MYCi361 (0~20μM; 5d) inhibited the viability of MYC-dependent cancer cells including prostate cancer (Myc-CaP, LNCaP, and PC3), leukemia (MV4-11), lymphoma (HL-60 and P493-6), and neuroblastoma (SK-N-B2) [1]. MYCi361 (6μM; 24h) inhibited the cell proliferation of primary prostate cancer cells [2].
MYCi361 (50mg/kg; bid; 2d; i.p.) induced tumor regression in FVB mice bearing established MycCaP tumor [1]. MYCi361 (55mg/kg; 42d; i.p.) significant decreased the tumor’s size and weight in NOD/SCID/IL2rg-/-(NSG) mice transplanted prostate cancer tumor tissues [2].
References:
[1] Han H, Jain A D, Truica M I, et al. Small-molecule MYC inhibitors suppress tumor growth and enhance immunotherapy [J]. Cancer Cell, 2019, 36(5): 483-97.e15.
[2] Ding T, Zhu Y, Jin H, et al. Circular RNA circ_0057558 controls prostate cancer cell proliferation through regulating miR-206/USP33/c-Myc axis [J]. Frontiers in cell and developmental biology, 2021, 9: 644397.
| Cell experiment [1]: | |
Cell lines | Primary prostate cancer cells |
Preparation Method | The cells were plated onto 96-well plates, cultured overnight, and then treated with 6µM MYCi361 or vehicle (DMSO). After 48h of culture, CCK-8 reagent was added and incubated at 37℃, 5% CO2 for another 1h. The optical density was recorded at 450nm (OD450) using a microplate reader. The inhibition rate of cell proliferation was calculated. |
Reaction Conditions | 6μM; 24h |
Applications | MYCi361 inhibited the cell proliferation of primary prostate cancer cells. |
| Animal experiment [2]: | |
Animal models | Male FVB mice |
Preparation Method | MycCaP Ebox-Luc cells suspended in 100ml BD matrigel were subcutaneously injected into flanks of mice to establish MycCaP allograft prostate mouse model. MYCi361 was dissolved in PBS with 10% DMSO and 20% Tween 80. Then the mice were treated with MYCi361 initially at 50mg/kg twice daily for 2 days. Caliper measurement of tumor size were performed after treatment. |
Dosage form | 50mg/kg; bid; 2d; i.p. |
Applications | MYCi361 induced tumor regression in FVB mice bearing established MycCaP tumor. |
References: | |
| Cas No. | 2289690-31-7 | SDF | |
| Synonyms | NUCC-0196361 | ||
| Canonical 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 | ||
| Formula | C26H16ClF9N2O2 | M.Wt | 594.86 |
| Solubility | DMSO: 110 mg/mL (184.92 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6811 mL | 8.4053 mL | 16.8107 mL |
| 5 mM | 336.2 μL | 1.6811 mL | 3.3621 mL |
| 10 mM | 168.1 μL | 840.5 μL | 1.6811 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 27 reference(s) in Google Scholar.)