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SB273005

Cat. No. M20604
SB273005 Structure
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Biological Activity

SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.

Chemical Information
Molecular Weight 451.44
Formula C22H24F3N3O4
CAS Number 205678-31-5
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Sbastien Rinaldetti, et al. Int J Mol Sci. High-Content Drug Discovery Targeting Molecular Bladder Cancer Subtypes

[2] Takuro Hirano, et al. Oncogenesis. FARP1 boosts CDC42 activity from integrin αvβ5 signaling and correlates with poor prognosis of advanced gastric cancer

[3] Shaobo Wang, et al. Cell Rep. Integrin αvβ5 Internalizes Zika Virus during Neural Stem Cells Infection and Provides a Promising Target for Antiviral Therapy

[4] Irena Horwacik, et al. Int J Oncol. Modulation of interactions of neuroblastoma cell lines with extracellular matrix proteins affects their sensitivity to treatment with the anti-GD2 ganglioside antibody 14G2a

[5] Deidre A Dalmas Wilk, et al. Toxicol In Vitro. In vitro investigation of integrin-receptor antagonist-induced vascular toxicity in the mouse

Related Integrin Products
HSDVHK-NH2

HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM).

LDV

LDV, a tripeptide, is a non-fluorescent analog of LDV-FITC.

Cyclo(RADfK)

Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis.

Obtustatin

Obtustatin is a non-RGD disintegrin of 41 residues.

Integrin Binding Peptide

Integrin Binding Peptide is derived by fibronectin.

  Catalog
Abmole Inhibitor Catalog




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