WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H407934
CAS#: 2207569-08-0
Description: QCA570 is 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. 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.
Hodoodo Cat#: H407934
Name: QCA570
CAS#: 2207569-08-0
Chemical Formula: C39H33N7O4S
Exact Mass: 695.23
Molecular Weight: 695.798
Elemental Analysis: C, 67.32; H, 4.78; N, 14.09; O, 9.20; S, 4.61
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Synonym: QCA570; QCA-570; QCA 570;
IUPAC/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
InChi Key: RTVTYLRQKKDYMQ-UHFFFAOYSA-N
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)
SMILES Code: O=C(C(N(CC1=C2C=CC=C1C#CCCCN3N=CC(C#CC(S4)=C(CC5=CC=CC=C5)C6=C4N7C(COC6)=NN=C7C)=C3)C2=O)CC8)NC8=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Proteins of the bromodomain and extra-terminal (BET) family are epigenetics "readers" and promising therapeutic targets for cancer and other human diseases.
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 695.80 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Qin C, Hu Y, Zhou B, Fernandez-Salas E, Yang CY, Liu L, McEachern D,
Przybranowski S, Wang M, Stuckey J, Meagher J, Bai L, Chen Z, Lin M, Yang J,
Ziazadeh DN, Xu F, Hu J, Xiang W, Huang L, Li S, Wen B, Sun D, Wang S. 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. doi: 10.1021/acs.jmedchem.8b00506. Epub 2018 Jul 18. PubMed
PMID: 30019901.