1. Cytoskeleton
  2. Integrin
  3. SB-267268

SB-267268 

Cat. No.: HY-19306
Handling Instructions

SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.

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SB-267268 Chemical Structure

SB-267268 Chemical Structure

CAS No. : 205678-26-8

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Description

SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression[1].

In Vitro

SB-267268 was much less potent for inhibition of human, mouse, and ratαvβ6 integrin. SB-267268 inhibits the attachment of bothαvβ3-transfected HEK293 cells to microtiter plate wells precoated with arginine-glycine-aspartic acid (RGD)-containing matrix proteins with IC50 values of 12 nM. SB-267268 also inhibits vitronectin-mediated human and rat aortic smooth-muscle-cell (SMC) migration with IC50 values of approximately 12.3 nM and 3.6 nM, respectively[1].

In Vivo

SB-267268 (60 mg/kg; bi-daily, i.p.) reduces blood vessel profiles (BVPs) in the inner retina by 50%[1].
In ROP mice treated with SB-267268, VEGF and VEGFR-2 gene expression in the inner nuclear layer (INL) and the ganglion cell layer (GCL) is reduced[1].

Animal Model: Pregnant female C57BL/6 mice (ROP mice)[1]
Dosage: 60 mg/kg
Administration: I.p.; bi-daily
Result: Reduced blood vessel profiles (BVPs) in the inner retina by 50%.
Molecular Weight

451.44

Formula

C₂₂H₂₄F₃N₃O₄

CAS No.

205678-26-8

SMILES

O=C(O)C[[email protected]]1C(N(CC(F)(F)F)CC2=CC(OCCCNC3=NC=CC=C3)=CC=C2C1)=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

SB-267268SB267268SB 267268Integrinnonpeptidicretinopathyprematurityanti-angiogenicischemicretinalpathologiesInhibitorinhibitorinhibit

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