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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
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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 406.47
Formula C21H30N2O6
CAS Number 238750-77-1
Purity 99.37%
Solubility DMSO 31 mg/mL
Storage at -20°C
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
Abmole Inhibitor Catalog




Keywords: Tosedostat, CHR2797 supplier, Aminopeptidase, inhibitors

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