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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.
| 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.
| Molecular Weight | 406.47 |
| Formula | C21H30N2O6 |
| CAS Number | 238750-77-1 |
| Purity | 99.37% |
| Solubility | DMSO 31 mg/mL |
| Storage | at -20°C |
| Related Aminopeptidase Products |
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| Firibastat
Firibastat (QGC001) is an orally active EC33 precursor drug. Firibastat is A first-in-class (first-in-class) brain aminopeptidase A (APA) inhibitor (Ki=200 nM) that selectively and specifically inhibits the conversion of cerebral angiotensin II to angiotensin III and lowers blood pressure in hypertensive rats. |
| LTA4H-IN-1
LTA4H metalloenzyme inhibitor LYS006 is a selective oral agent in multiple Ph.II studies for the study of inflammatory diseases, including ulcerative colitis and NASH. |
| Bestatin hydrochloride
Bestatin hydrochloride is an inhibitor of CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase, used for cancer research. |
| Ubenimex
Ubenimex, also known as bestatin, is a competitive protease inhibitor. |
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