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ARV-825 - 97%, high purity , CAS No.1818885-28-7

COA COA
    Grade & Purity:
  • ≥97%
In stock
Item Number
A413965
Grouped product items
SKU Size
Availability
 Price Qty
A413965-1mg
1mg
2
$49.90
A413965-5mg
5mg
2
$129.90
A413965-10mg
10mg
2
$159.90
A413965-25mg
25mg
1
$259.90
A413965-50mg
50mg
1
$353.90
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PROTAC

View related series
Epigenetic Reader Domain (314) Epigenetics (1496) Hydroxy PEG (472) Lipid PEG (395) PROTAC (2077) PROTAC linker (720) PROTAC Linkers (1898) PROTACs (183) Tetrazine-PEG (145)

Basic Description

Synonyms 6H-​Thieno[3,​2-​f]​[1,​2,​4]​triazolo[4,​3-​a]​[1,​4]​diazepine-​6-​acetamide,4-​(4-​chlorophenyl)​-​N-​[4-​[2-​[2-​[2-​[2-​[[2-​(2,​6-​dioxo-​3-​piperidinyl)​-​2,​3-​dihydro-​1,​3-​dioxo-​1H-​isoindol-​4-​yl]​amino]​ethoxy]​ethoxy]​ethoxy]​ethoxy]​phen
Specifications & Purity ≥97%
Biochemical and Physiological Mechanisms ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description

Information

ARV-825 is a BRD4 Inhibitor that recruits BRD4 to the E3 ubiquitin ligase cereblon, leading to fast, efficient, and prolonged degradation of BRD4 and sustained down-regulation of MYC.


Targets

BRD4 BD2 (Cell-free assay); BRD4 BD1 (Cell-free assay) 28 nM(Kd); 90 nM(Kd)


In vitro

Compared with the BRD4 inhibitors, ARV-825 treatment results in a strikingly more pronounced effect on the levels of c-MYC, and downstream cell proliferation and apoptosis induction in BL (Burkitt’s Lymphoma) cell lines. The IC50s of ARV-825 for all tested cell lines and primary AML cells at 72 hours are in the low nanomolar range (2-50 nM). ARV-825 treatment reduces PIM1 levels and phosphorylation of CXCR4 in AML cells while overexpression of PIM1 or Myc reverses the phenomena.


In vivo

In a mouse model of human leukemia, the leukemia burdens are significantly lower in the ARV-825 treated mice as confirmed by luciferase imaging, flow cytometry, spleen size and survived longer compared to control mice.


Cell Research(from reference)

Cell lines：RS4;11 cells 

Concentrations：3, 10, 30 nM 

Incubation Time：3 h 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Isoindoles and derivatives
Subclass Isoindolines
Intermediate Tree Nodes Isoindolones
Direct Parent Phthalimides
Alternative Parents Alpha amino acids and derivatives  Thienodiazepines  Anilides  Isoindoles  N-arylamides  Phenol ethers  Phenoxy compounds  Piperidinediones  Secondary alkylarylamines  Alkyl aryl ethers  Chlorobenzenes  Delta lactams  1,4-diazepines  Aryl chlorides  N-substituted carboxylic acid imides  Vinylogous amides  Triazoles  Dicarboximides  Heteroaromatic compounds  Thiophenes  N-unsubstituted carboxylic acid imides  Secondary carboxylic acid amides  Ketimines  Dialkyl ethers  Propargyl-type 1,3-dipolar organic compounds  Azacyclic compounds  Organic oxides  Organochlorides  Carbonyl compounds  Hydrocarbon derivatives  Organopnictogen compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Phthalimide - Thieno-para-diazepine - Alpha-amino acid or derivatives - Isoindole - Anilide - Piperidinedione - Phenoxy compound - Phenol ether - N-arylamide - Piperidinone - Secondary aliphatic/aromatic amine - Para-diazepine - Alkyl aryl ether - Halobenzene - Delta-lactam - Chlorobenzene - Aryl halide - Benzenoid - Monocyclic benzene moiety - Piperidine - Aryl chloride - Carboxylic acid imide, n-substituted - Azole - Heteroaromatic compound - Carboxylic acid imide - Vinylogous amide - Dicarboximide - 1,2,4-triazole - Carboxylic acid imide, n-unsubstituted - Thiophene - Secondary carboxylic acid amide - Lactam - Ketimine - Carboxamide group - Amino acid or derivatives - Secondary amine - Propargyl-type 1,3-dipolar organic compound - Carboxylic acid derivative - Azacycle - Dialkyl ether - Ether - Organic 1,3-dipolar compound - Hydrocarbon derivative - Carbonyl group - Organic oxygen compound - Organic nitrogen compound - Organic oxide - Organopnictogen compound - Organooxygen compound - Amine - Organonitrogen compound - Imine - Organochloride - Organohalogen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as phthalimides. These are aromatic heterocyclic compounds containing a 1,3-dioxoisoindoline moiety. They are imide derivatives of phthalic anhydrides.
External Descriptors Not available

Associated Targets(Human)

BRD4 Tchem Bromodomain-containing protein 4 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CRBN Tclin Protein cereblon (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
HL-60 (67320 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MV4-11 (7307 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RS4-11 (1012 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MOLM-13 (2241 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CRBN Tclin Protein cereblon (139 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CRBN Tclin Cereblon/Ikaros (139 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Cereblon/Cullin-4A/Bromodomain-containing protein 4 (37 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD2 Tchem Cereblon/Cullin-4A/Bromodomain-containing protein 2 (31 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD3 Tchem Cereblon/Cullin-4A/Bromodomain-containing protein 3 (31 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Cereblon/Bromodomain-containing protein 4 (275 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem von Hippel-Lindau disease tumor suppressor/Bromodomain-containing protein 4 (105 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem von Hippel-Lindau disease tumor suppressor/Elongin-B/Elongin-C/Bromodomain-containing protein 4 (54 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD2 Tchem von Hippel-Lindau disease tumor suppressor/Elongin-B/Elongin-C/Bromodomain-containing protein 2 (24 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD3 Tchem von Hippel-Lindau disease tumor suppressor/Elongin-B/Elongin-C/Bromodomain-containing protein 3 (22 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name 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]-N-[4-[2-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]ethoxy]phenyl]acetamide
INCHI InChI=1S/C46H47ClN8O9S/c1-26-27(2)65-46-39(26)41(29-7-9-30(47)10-8-29)50-35(42-53-52-28(3)54(42)46)25-38(57)49-31-11-13-32(14-12-31)64-24-23-63-22-21-62-20-19-61-18-17-48-34-6-4-5-33-40(34)45(60)55(44(33)59)36-15-16-37(56)51-43(36)58/h4-14,35-36,48H,15-25H2,1-3H3,(H,49,57)(H,51,56,58)/t35-,36?/m0/s1
InChIKey RWLOGRLTDKDANT-TYIYNAFKSA-N
Smiles CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)OCCOCCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)C8=CC=C(C=C8)Cl)C
Isomeric SMILES CC1=C(SC2=C1C(=N[C@H](C3=NN=C(N32)C)CC(=O)NC4=CC=C(C=C4)OCCOCCOCCOCCNC5=CC=CC6=C5C(=O)N(C6=O)C7CCC(=O)NC7=O)C8=CC=C(C=C8)Cl)C
Molecular Weight 923.43
Reaxy-Rn 29518940
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29518940&ln=

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

10 results found

Lot Number Certificate Type Date Item
E2422391 Certificate of Analysis Feb 26, 2024 A413965
E2422393 Certificate of Analysis Feb 26, 2024 A413965
E2422384 Certificate of Analysis Feb 26, 2024 A413965
E2422386 Certificate of Analysis Feb 26, 2024 A413965
E2422387 Certificate of Analysis Feb 26, 2024 A413965
E2422388 Certificate of Analysis Feb 26, 2024 A413965
E2422389 Certificate of Analysis Feb 26, 2024 A413965
E2422390 Certificate of Analysis Feb 26, 2024 A413965
E2422392 Certificate of Analysis Feb 26, 2024 A413965
E2422396 Certificate of Analysis Feb 26, 2024 A413965

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 100 mg/mL (108.29 mM); Ethanol: 3 mg/mL (3.24 mM); Water: Insoluble;
Molecular Weight 923.400 g/mol
XLogP3 4.800
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 14
Rotatable Bond Count 19
Exact Mass 922.288 Da
Monoisotopic Mass 922.288 Da
Topological Polar Surface Area 233.000 Ų
Heavy Atom Count 65
Formal Charge 0
Complexity 1720.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 1
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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