QCA570 |
カタログ番号GC33217
One-Click Copy Product Info
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QCA570 は、BRD4 BD1 タンパク質の IC50 が 10 nM で、Cereblon と BET のリガンドによって接続された PROTAC です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2207569-08-0
Sample solution is provided at 25 µL, 10mM.
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QCA570 is a potent BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein.
QCA570 is an extremely potent and highly efficacious BET degrader, capable of degrading BET proteins at low picomolar (pM) concentrations in leukemia cells. QCA570 inhibits cell growth in MV4;11, MOLM-13, and RS4;11 cell lines with IC50 values of 8.3, 62, and 32 pM, respectively. QCA570 is the most potent and efficacious BET degrader reported to date[1].
[1]. Qin C, et al. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704.
Animal experiment: | Mice[1]Female SCID mice bearing RS4;11 xenograft tumors were dosed with a single intravenous dose of QCA570 (compound 35) at 5 mg/kg[1]. |
References: [1]. Qin C, et al. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 Aug 9;61(15):6685-6704. | |
| Cas No. | 2207569-08-0 | SDF | |
| Canonical SMILES | O=C(N(C1CCC(NC1=O)=O)C2)C3=C2C(C#CCCCN4N=CC(C#CC(S5)=C(CC6=CC=CC=C6)C(COC7)=C5N8C7=NN=C8C)=C4)=CC=C3 | ||
| Formula | C39H33N7O4S | M.Wt | 695.79 |
| 溶解度 | Soluble in DMSO | Storage | -20°C, protect from light |
| 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 | 1.4372 mL | 7.1861 mL | 14.3722 mL |
| 5 mM | 287.4 μL | 1.4372 mL | 2.8744 mL |
| 10 mM | 143.7 μL | 718.6 μL | 1.4372 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: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 31 reference(s) in Google Scholar.)