SIAIS100 TFA |
カタログ番号GC73377
One-Click Copy Product Info
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SIAIS100 TFAはdc50値2.7 nmの強力なbcr-abl protac分解剤です。
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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SIAIS100 TFA is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 TFA can be used to research chronic myeloid leukemia (CML).
SIAIS100 exhibits anti-proliferative activity against K562 cells with an IC50 value of 12 nM[1].SIAIS100 degrades BCR-ABL with degradation ratio of 81.78% and 91.20% at 5 nM and 100 nM, respectively[1].SIAIS100 (100 nM; 8 h) significantly decreases BCR-ABL in K562 cells[1].SIAIS100 (100 nM; 6 h) induced sustained and robust BCR-ABL degradation and maintained a durable cellular response after drug removal[1].SIAIS100 (1-1000 nM) significantly degrade mutation G250E/T315I dose-dependently accompanied by the inhibition of BCR-ABL signaling assessed by the level of p-BCR-ABL in 32D cells[1].
References:
[1]. Liu H, et al. Discovery and characterization of novel potent BCR-ABL degraders by conjugating allosteric inhibitor. Eur J Med Chem. 2022 Dec 15;244:114810.
| Cas No. | SDF | ||
| Formula | C46H51ClF5N9O7S | M.Wt | 1004.46 |
| 溶解度 | DMSO : 100 mg/mL (99.56 mM; Need ultrasonic) | Storage | -20°C, stored under nitrogen, away from moisture |
| 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 | 995.6 μL | 4.9778 mL | 9.9556 mL |
| 5 mM | 199.1 μL | 995.6 μL | 1.9911 mL |
| 10 mM | 99.6 μL | 497.8 μL | 995.6 μL |
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.)