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AB285434

AZD-5069

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MW 476.5 Da, Purity >98%. A potent and reversible CXCR2 chemokine receptor antagonist with potential anti-inflammatory and antineoplastic activities. Upon administration, CXC chemokine receptor 2 antagonist AZD5069 directly binds to CXCR2 and inhibits its activation. This inhibits CXCR2-mediated signaling and may inhibit tumor cell proliferation in CXCR2-overexpressing tumor cells.

View Alternative Names

C C, C-C CKR-1, C-X-C chemokine receptor type 1, C-X-C chemokine receptor type 2, CD 181, CD 182, CD128, CD181 antigen, CD182 antigen, CDw128a, CDw128b, CKR 1, CMKAR1, CMKAR2, CXCR1_HUMAN, CXCR2_HUMAN, Chemokine (C X C motif) receptor 1, Chemokine (C X C) receptor 1, Chemokine (CXC) receptor 2, Chemokine receptor 1, GRO/MGSA receptor, High affinity interleukin-8 receptor A, High affinity interleukin-8 receptor B, IL-8 receptor type 1, IL-8 receptor type 2, IL-8R A, IL-8R B, IL8 receptor, IL8R1, IL8R2, IL8RBA, Interleukin 8 Receptor B, Interleukin 8 receptor alpha, Interleukin 8 receptor type 1, Interleukin 8 receptor type A, Interleukin 8 receptor, beta, Interleukin 8 receptor, type 2

Key facts

CAS number

878385-84-3

Purity

>98%

Form

Solid

form

Molecular weight

476.5 Da

Molecular formula

C<sub>1</sub><sub>8</sub>H<sub>2</sub><sub>2</sub>F<sub>2</sub>N<sub>4</sub>O<sub>5</sub>S<sub>2</sub>

PubChem

56645576

Nature

Synthetic

Solubility

Soluble in DMSO

Biochemical name

N-(2-((2,3-difluorobenzyl)thio)-6-(((2R,3S)-3,4-dihydroxybutan-2-yl)oxy)pyrimidin-4-yl)azetidine-1-sulfonamide

Biological description

A potent and reversible CXCR2 chemokine receptor antagonist with potential anti-inflammatory and antineoplastic activities. Upon administration, CXC chemokine receptor 2 antagonist AZD5069 directly binds to CXCR2 and inhibits its activation. This inhibits CXCR2-mediated signaling and may inhibit tumor cell proliferation in CXCR2-overexpressing tumor cells.

Canonical smiles

CC(C(CO)O)OC1=NC(=NC(=C1)NS(=O)(=O)N2CCC2)SCC3=C(C(=CC=C3)F)F

Isomeric smiles

C[C@H]([C@H](CO)O)OC1=NC(=NC(=C1)NS(=O)(=O)N2CCC2)SCC3=C(C(=CC=C3)F)F

InChi

InChI=1S/C18H22F2N4O5S2/c1-11(14(26)9-25)29-16-8-15(23-31(27,28)24-6-3-7-24)21-18(22-16)30-10-12-4-2-5-13(19)17(12)20/h2,4-5,8,11,14,25-26H,3,6-7,9-10H2,1H3,(H,21,22,23)/t11-,14+/m1/s1

InChiKey

QZECRCLSIGFCIO-RISCZKNCSA-N

IUPAC Name

N-[2-[(2,3-difluorophenyl)methylsulfanyl]-6-[(2R,3S)-3,4-dihydroxybutan-2-yl]oxypyrimidin-4-yl]azetidine-1-sulfonamide

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Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2053 AZD-5069. B2053-25 is the same size as the 25 mg size of ab285434.
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Properties and storage information

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
This product is air and light sensitive and impurities can occur as a result of air oxidation or due to metabolism by microbes
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

CXCR1 and CXCR2 also known as IL8RA and IL8RB respectively are G-protein coupled receptors with an important role in chemokine binding. These receptors are expressed predominantly on the surface of neutrophils but also appear on monocytes and some endothelial cells. They have a mass of approximately 46 kDa. Mechanically these receptors facilitate the response to chemokines like IL-8 which leads to neutrophil activation and migration towards sites of inflammation.
Biological function summary

The receptors interact with interleukin-8 to mediate immune responses. They form part of a heterotrimeric complex with G-proteins triggering downstream signaling events. Activation of CXCR1 and CXCR2 recruits neutrophils to infection sites facilitating the innate immune response. They contribute to processes such as chemotaxis degranulation and regulation of ROS production highlighting their role in managing acute inflammation.

Pathways

These receptors are key players in the chemokine signaling pathway and inflammatory response pathway. The binding of chemokines to CXCR1 and CXCR2 activates downstream proteins such as those from the MAPK cascade. Their signaling is closely linked with proteins like GRK2 which regulates receptor desensitization and PI3K important for intracellular signal transduction.

The receptors have associations with disorders like asthma and chronic obstructive pulmonary disease (COPD). Dysregulation of CXCR1 and CXCR2 signaling can lead to excessive neutrophilic infiltration exacerbating these diseases. The receptors also interact with proteins like IL-8 where elevated levels can drive persistent inflammation highlighting their potential as therapeutic targets in inflammatory disorders.
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Product protocols

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Complementary Products

Biochemicals

AB120895

SB 225002, non-peptide CXCR2 antagonist

Chemical Structure - SB 225002, non-peptide CXCR2 antagonist (AB120895)

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Assay Kits

AB65348

NAD/NADH Assay Kit (Colorimetric)

Biochemical assay - NAD/NADH Assay Kit (Colorimetric) (AB65348)

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Primary Antibodies

AB9332

Anti-Phosphoserine antibody

Western blot - Anti-Phosphoserine antibody (AB9332)

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Proteins & Peptides

AB112309

Recombinant Human CXCR2 protein

SDS-PAGE - Recombinant Human CXCR2 protein (AB112309)

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