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Tosedostat

Cat. No. M2284
Tosedostat Structure
Synonym:

CHR2797

Size Price Availability Quantity
2mg USD 85  USD85 In stock
5mg USD 150  USD150 In stock
10mg USD 235  USD235 In stock
25mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

Tosedostat (CHR2797) is an aminopeptidase inhibitor with IC50 of 100, 150, 220, <1000, <5000, <10000 and <30000 nM for LAP, PuSA, aminopeptidase N, aminopeptidase B, PILSAP, LTA4 hydrolase and MetAP2, respectively. It has demonstrated anti-tumour activity in a number of models of cancer, both as a single agent and in synergy with cytotoxic agents such as carboplatin and paclitaxel.

Chemical Information
Molecular Weight 406.47
Formula C21H30N2O6
CAS Number 238750-77-1
Solubility (25°C) DMSO 31 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] Jeroen Janssen, et al. Inferior Outcome of Addition of the Aminopeptidase Inhibitor Tosedostat to Standard Intensive Treatment for Elderly Patients with AML and High Risk MDS

[2] Patrick Grierson, et al. Phase Ib/II study combining tosedostat with capecitabine in patients with advanced pancreatic adenocarcinoma

[3] Rohit Singh, et al. Discovery of Anticancer Clinical Candidate, Tosedostat, As an Analgesic Agent

[4] Courtney D DiNardo, et al. Tosedostat for the treatment of relapsed and refractory acute myeloid leukemia

[5] Michael S Mathisen, et al. Efficacy of tosedostat, a novel, oral agent for elderly patients with relapsed or refractory acute myeloid leukemia: a review of the Phase II OPAL trial

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  Catalog
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Keywords: Tosedostat, CHR2797 supplier, Aminopeptidase, inhibitors, activators


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