| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
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Purity: ≥98%
QCA570 is an highly potent and efficacious BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein. QCA570 achieves complete and durable tumor regression in leukemia xenograft models in mice at well-tolerated dose-schedules. QCA570 is the most potent and efficacious BET degrader reported to date.
| ln Vitro |
In leukemia cells, QCA570 is a very strong and effective BET degrader that can break down BET proteins at low picomolar (pM) concentrations. MV4;11, MOLM-13, and RS4;11 cell lines are all inhibited in terms of cell growth by QCA570, with IC50 values of 8.3, 62, and 32 pM, respectively. The most successful BET degrader discovered to far is QCA570 [1].
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| References |
| Molecular Formula |
C39H33N7O4S
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|---|---|
| Molecular Weight |
695.788826704025
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| Exact Mass |
695.231
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| CAS # |
2207569-08-0
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| PubChem CID |
134348221
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| Appearance |
White to off-white solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
51
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| Complexity |
1460
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(C#CC2C=NN(C=2)CCCC#CC2=CC=CC3C(N(CC=32)C2C(NC(CC2)=O)=O)=O)=C(CC2C=CC=CC=2)C2COCC3=NN=C(C)N3C1=2
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| InChi Key |
RTVTYLRQKKDYMQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C39H33N7O4S/c1-25-42-43-35-24-50-23-32-30(19-26-9-4-2-5-10-26)34(51-39(32)46(25)35)16-14-27-20-40-44(21-27)18-7-3-6-11-28-12-8-13-29-31(28)22-45(38(29)49)33-15-17-36(47)41-37(33)48/h2,4-5,8-10,12-13,20-21,33H,3,7,15,17-19,22-24H2,1H3,(H,41,47,48)
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| Chemical Name |
3-(4-(5-(4-((3-Benzyl-9-methyl-4H,6H-thieno[2,3-e][1,2,4]-triazolo[3,4-c][1,4]oxazepin-2-yl)ethynyl)-1H-pyrazol-1-yl)pent-1-yn-1-yl)-1-oxoisoindolin-2-yl)piperidine-2,6-dione
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| Synonyms |
QCA570 QCA-570 QCA 570
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~40 mg/mL (~57.49 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (2.87 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (2.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4372 mL | 7.1861 mL | 14.3722 mL | |
| 5 mM | 0.2874 mL | 1.4372 mL | 2.8744 mL | |
| 10 mM | 0.1437 mL | 0.7186 mL | 1.4372 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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