AP-1 |
| Katalog-Nr.GC91040 |
Ein PROTAC, der den Abbau von ALK fördert.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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AP-1 is a miniaturized proteolysis-targeting chimera (PROTAC) that contains an anaplastic lymphoma kinase (ALK) ligand connected to the E3 ubiquitin ligase ligand (±)-thalidomide by an ultrashort linker.1 It degrades the ALK fusion protein NPM-ALK in Karpas-299 cells, where it is highly expressed, when used at concentrations ranging from 10 to 300 nM, an effect that can be blocked by the proteasome inhibitor MG-132. It also degrades the ALK fusion protein EML4-ALK and ALK containing the phenylalanine-to-leucine substitution mutation at position 1174 (ALKF1174L) expressed in SN-N-SH and NCI H3122 cells, respectively. AP-1 is cytotoxic to ALK-dependent Karpas-299 cells (IC50 = 0.1265 nM) but not non-ALK-dependent THP-1 cells (IC50 = 2,704 nM). It reduces tumor volume in an NCI H3122 mouse xenograft model when administered at doses of 25, 50, and 100 mg/kg.
| Cas No. | SDF | ||
| Formula | C39H40ClN9O8S | M.Wt | 830.3 |
| Löslichkeit | DMF: 30 mg/ml,DMSO: 30 mg/ml | 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. |
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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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2044 mL | 6.0219 mL | 12.0438 mL |
| 5 mM | 0.2409 mL | 1.2044 mL | 2.4088 mL |
| 10 mM | 0.1204 mL | 0.6022 mL | 1.2044 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 ddH2O, 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: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
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