| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
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| 5mg |
|
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| 10mg | |||
| Other Sizes |
| Targets |
BRD4 6 nM (DC50) BRD2 1 nM (DC50) BRD3 4 nM (DC50) VHL
BET family bromodomains (BRD2, BRD3, BRD4). |
|---|---|
| ln Vitro |
OARV-771 exhibits an antiproliferative effect with an EC50 value of 4 nM in MV4;11[1]
OARV-771 demonstrates potent degradation of BET proteins with DC50 values of 1 nM for BRD2, 4 nM for BRD3, and 6 nM for BRD4 in cellular assays. The compound exhibits improved cell permeability compared to earlier BET degraders, enabling more efficient target engagement and protein degradation at lower concentrations in various cancer cell lines. |
| ln Vivo |
No specific in vivo data found; please refer to general properties of BET degraders: PROTACs like ARV-771 typically demonstrate potent antitumor efficacy in xenograft mouse models at well-tolerated doses, with significant tumor growth inhibition and target protein degradation observed in tumor tissues following intraperitoneal (IP) or intravenous (IV) administration.
|
| Enzyme Assay |
Assay: In vitro biochemical binding and degradation assays. Protocol: Recombinant BET bromodomain proteins are incubated with varying concentrations of OARV-771 in the presence of VHL E3 ligase complex. Degradation is measured via time-resolved FRET (TR-FRET) or AlphaScreen technology to quantify ternary complex formation and subsequent ubiquitination efficiency.
|
| Cell Assay |
Cells: Various cancer cell lines (e.g., HeLa, HFF-1, HCCLM3, MDA-MB-231). Protocol: Cells are treated with OARV-771 at concentrations ranging from 1 nM to 1 microM for 16-24 hours. Protein levels of BRD2, BRD3, and BRD4 are analyzed by Western blotting. Cell viability is assessed via CCK-8 or MTT assays after 72 hours of treatment.
|
| Animal Protocol |
No specific in vivo protocol found; please refer to general BET degrader protocols: Typical administration is via intraperitoneal (IP) injection in xenograft mouse models, with doses ranging from 10 to 50 mg/kg administered daily or every other day. Tumor volume and body weight are monitored, and tumor tissues are collected for Western blot analysis of target degradation.
|
| ADME/Pharmacokinetics |
No specific data found; please refer to general BET degrader properties: PROTAC molecules generally exhibit moderate to good oral bioavailability but are often administered via IP injection in preclinical studies. They typically show short half-lives due to rapid clearance, but degradation activity can persist beyond the compound's presence in circulation.
|
| Toxicity/Toxicokinetics |
No specific data found; please refer to general BET degrader properties: Generally well-tolerated at efficacious doses in preclinical models, with no significant body weight loss or major organ toxicity observed. Off-target degradation of other bromodomain-containing proteins may occur at higher concentrations and should be carefully monitored.
|
| References | |
| Additional Infomation |
OARV-771 was developed as a research tool to study BET protein biology using targeted protein degradation technology. The VHL-based design provides enhanced cell permeability compared to early-generation degraders. The compound is not approved for clinical use and is strictly intended for laboratory research applications.
|
| Molecular Formula |
C49H59CLN8O8S2
|
|---|---|
| Molecular Weight |
987.624568223953
|
| Exact Mass |
986.358
|
| CAS # |
2683008-37-7
|
| PubChem CID |
162679304
|
| Appearance |
White to off-white solid powder
|
| LogP |
6.4
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
14
|
| Rotatable Bond Count |
20
|
| Heavy Atom Count |
68
|
| Complexity |
1750
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
CC1=C(SC2N3C(=NN=C3[C@H](CC(=O)OCCOCCCOCC(=O)N[C@@H](C(C)(C)C)C(N3C[C@H](O)C[C@H]3C(=O)N[C@H](C3C=CC(C4=C(N=CS4)C)=CC=3)C)=O)N=C(C3C=CC(Cl)=CC=3)C1=2)C)C
|
| InChi Key |
CWTFXHWWWKKEQI-QQRWPDCKSA-N
|
| InChi Code |
InChI=1S/C49H59ClN8O8S2/c1-27-30(4)68-48-41(27)42(33-14-16-35(50)17-15-33)53-37(45-56-55-31(5)58(45)48)23-40(61)66-21-20-64-18-9-19-65-25-39(60)54-44(49(6,7)8)47(63)57-24-36(59)22-38(57)46(62)52-28(2)32-10-12-34(13-11-32)43-29(3)51-26-67-43/h10-17,26,28,36-38,44,59H,9,18-25H2,1-8H3,(H,52,62)(H,54,60)/t28-,36+,37-,38-,44+/m0/s1
|
| Chemical Name |
2-[3-[2-[[(2S)-1-[(2S,4R)-4-hydroxy-2-[[(1S)-1-[4-(4-methyl-1,3-thiazol-5-yl)phenyl]ethyl]carbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-2-oxoethoxy]propoxy]ethyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : 100 mg/mL (101.25 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 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: ≥ 2.5 mg/mL (2.53 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0125 mL | 5.0627 mL | 10.1254 mL | |
| 5 mM | 0.2025 mL | 1.0125 mL | 2.0251 mL | |
| 10 mM | 0.1013 mL | 0.5063 mL | 1.0125 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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