الصفحة الرئيسية>>Signaling Pathways>> PROTAC>>ARV-825

ARV-825

رقم الكتالوجGC19038

ARV-825 عبارة عن PROTAC متصل بواسطة روابط لـ Cereblon و BRD4يرتبط ARV-825 بـ BD1 و BD2 من BRD4 مع Kds من 90 و 28 نانومتر ، على التوالي

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ARV-825 التركيب الكيميائي

Cas No.: 1818885-28-7

الحجم السعر المخزون الكميّة
5mg
102٫00
متوفر
10mg
176٫00
متوفر
50mg
510٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of ARV-825

ARV-825 is a BRD4 Inhibitor based on PROTAC technology. ARV-825 binds to BD1 and BD2 of BRD4 with Kds of 90 and 28 nM, respectively.

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have Kds of 28-90 nM and ~3 uM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors[1].

References:
[1]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

Protocol of ARV-825

Kinase experiment:

Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscan by DiscoverX[1].

References:

[1]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63.

Chemical Properties of ARV-825

Cas No. 1818885-28-7 SDF
Canonical SMILES CC1=NN=C2N1C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NC5=CC=C(OCCOCCOCCOCCNC6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)C=C5)=O
Formula C46H47ClN8O9S M.Wt 923.43
الذوبان DMSO : ≥ 50 mg/mL (54.15 mM) Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ARV-825

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.0829 mL 5.4146 mL 10.8292 mL
5 mM 0.2166 mL 1.0829 mL 2.1658 mL
10 mM 0.1083 mL 0.5415 mL 1.0829 mL
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In vivo Formulation Calculator (Clear solution) of ARV-825

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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.
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Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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