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Toceranib phosphate

Cat. No. M20877
Toceranib phosphate Structure
Synonym:

SU11654

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Biological Activity

Toceranib phosphate is a multitargeted indolinone receptor tyrosine kinase (RTK) inhibitor with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively.

Chemical Information
Molecular Weight 494.45
Formula C22H28FN4O6P
CAS Number 874819-74-6
Solubility (25°C) DMSO 2 mg/mL
Water 2 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] Sabina Sheppard-Olivares, et al. Vet Rec Open. Toceranib phosphate in the management of canine insulinoma: A retrospective multicentre study of 30 cases (2009-2019)

[2] Petros Frezoulis, et al. Vet Comp Oncol. The role of toceranib phosphate in dogs with non-mast cell neoplasia: A systematic review

[3] Hiroki Yamazaki, et al. J Vet Intern Med. Assessment of postoperative adjuvant treatment using toceranib phosphate against adenocarcinoma in dogs

[4] Felicia H Lew, et al. Vet Comp Oncol. Retrospective evaluation of canine heart base tumours treated with toceranib phosphate (Palladia): 2011-2018

[5] C London, et al. Vet Comp Oncol. Preliminary evidence for biologic activity of toceranib phosphate (Palladia(®)) in solid tumours

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Keywords: Toceranib phosphate, SU11654 supplier, VEGFR/PDGFR, inhibitors, activators

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