F5446 |
Catalog No.GC73294
One-Click Copy Product Info
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F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 metltransferase.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2304465-89-0
Sample solution is provided at 25 µL, 10mM.
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F5446 (Compound 1) is a selective small molecule inhibitor of SUV39H1 metltransferase. F5446 decreases H3K9me3 deposition at the FAS promoter, increases Fas expression and increases colorectal carcinoma cell sensitivity to FasL-induced apoptosis in vitro. F5446 suppresses human colon tumor xenograft growth in vivo.
F5446 (0-1 μM, 2 days) has an EC50 of 4.96x10-7 M against recombinant human SUV39H1 and induces apoptotic cell death in the SW620 and LS411N cells[1].F5446 (0-250 nM, 3 days) up-regulates tumor cell surface Fas expression and increases FasL- induced apoptosis in SW620 and LS411N cells[1][2].F5446 (100 or 250 nM, 48 h) inhibits SUV39H1 expression and induces human colon tumor cell cycle arrest and apoptosis[2].
IF5446 (10 mg/kg, s.c.,every two days for 14 days) inhibits SUV39H1 and colon tumor growth at least in part through inhibiting H3K9me3 to increase the expression part through inhibiting H3K9me3 to increase the expression level of granzyme B , perforin , Fasl and IFNy in tumor-infiltrating CTLs in the tumor microenvironment in mice bearing MC38 and CT26 tumor[1][2].IF5446 (10 and 20 mg/kg, s.c.,every two days for 14 days) increases T-cell effector expression to suppress colon carcinoma growth[3].
References:
[1]. Chunwan Lu, et al. Small molecule histone metltransferase SUV39H1 inhibitor and uses thereof. US10577371B2. 2018. [2]. Lu C, et al. SUV39H1 regulates human colon carcinoma apoptosis and cell cycle to promote tumor growth. Cancer Lett. 2020 Apr 28;476:87-96.
[3]. Lu C, et al. SUV39H1 Represses the Expression of Cytotoxic T-Lymphocyte Effector Genes to Promote Colon Tumor Immune Evasion. Cancer Immunol Res. 2019 Mar;7(3):414-427.
| Cas No. | 2304465-89-0 | SDF | |
| Formula | C26H17ClN2O8S | M.Wt | 552.94 |
| Solubility | DMSO : 100 mg/mL (180.85 mM; Need ultrasonic) | Storage | -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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8085 mL | 9.0426 mL | 18.0851 mL |
| 5 mM | 361.7 μL | 1.8085 mL | 3.617 mL |
| 10 mM | 180.9 μL | 904.3 μL | 1.8085 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)