1. Cytoskeleton
  2. Integrin
  3. SB-267268

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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Based on 1 publication(s) in Google Scholar

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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].

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
12 nM
Compound: 5
HEK cell adhesion mediated by alpha v beta 3 integrin
HEK cell adhesion mediated by alpha v beta 3 integrin
[PMID: 10633035]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (443.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2151 mL 11.0757 mL 22.1513 mL
5 mM 0.4430 mL 2.2151 mL 4.4303 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2151 mL 11.0757 mL 22.1513 mL 55.3783 mL
5 mM 0.4430 mL 2.2151 mL 4.4303 mL 11.0757 mL
10 mM 0.2215 mL 1.1076 mL 2.2151 mL 5.5378 mL
15 mM 0.1477 mL 0.7384 mL 1.4768 mL 3.6919 mL
20 mM 0.1108 mL 0.5538 mL 1.1076 mL 2.7689 mL
25 mM 0.0886 mL 0.4430 mL 0.8861 mL 2.2151 mL
30 mM 0.0738 mL 0.3692 mL 0.7384 mL 1.8459 mL
40 mM 0.0554 mL 0.2769 mL 0.5538 mL 1.3845 mL
50 mM 0.0443 mL 0.2215 mL 0.4430 mL 1.1076 mL
60 mM 0.0369 mL 0.1846 mL 0.3692 mL 0.9230 mL
80 mM 0.0277 mL 0.1384 mL 0.2769 mL 0.6922 mL
100 mM 0.0222 mL 0.1108 mL 0.2215 mL 0.5538 mL
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SB-267268 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
SB-267268
Cat. No.:
HY-19306
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