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Cilengitide trifluoroacetate

Cat. No. M9173
Cilengitide trifluoroacetate Structure
Synonym:

EMD 121974; NSC 707544

Size Price Availability Quantity
5mg USD 50  USD50 In stock
2mg USD 80  USD80 In stock
10mg USD 130  USD130 In stock
25mg USD 260  USD260 In stock
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Quality Control & Documentation
Biological Activity

Cilengitide is a potent integrin inhibitor for αvβ3 receptor and αvβ5 receptor with IC50 of 4.1 nM and 79 nM in cell-free assays, respectively ~10-fold selectivity against gpIIbIIIa.

Product Citations
Chemical Information
Molecular Weight 703
Formula C29H41F3N8O9
CAS Number 199807-35-7
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] Young-Hoon Kim, et al. Int J Cancer . Combination therapy of cilengitide with belotecan against experimental glioblastoma

[2] Timo L M Ten Hagen, et al. Int J Cancer. The αVβ3/αVβ5 integrin inhibitor cilengitide augments tumor response to melphalan isolated limb perfusion in a sarcoma model

[3] S Hariharan, et al. Ann Oncol . Assessment of the biological and pharmacological effects of the alpha nu beta3 and alpha nu beta5 integrin receptor antagonist, cilengitide (EMD 121974), in pаtιепts with advanced solid tumors

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  Catalog
Abmole Inhibitor Catalog




Keywords: Cilengitide trifluoroacetate, EMD 121974; NSC 707544 supplier, Integrin, inhibitors, activators


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