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Tasisulam sodium

Cat. No. M30230
Tasisulam sodium Structure
Synonym:

LY 573636 sodium

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Biological Activity

Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization.

Chemical Information
Molecular Weight 437.09
Formula C11H5BrCl2NNaO3S2
CAS Number 519055-63-1
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Yutaka Fujiwara, et al. Cancer Chemother Pharmacol. A phase I study of tasisulam sodium using an albumin-tailored dose in Japanese patients with advanced solid tumors

[2] Giorgio V Scagliotti, et al. J Thorac Oncol. Tasisulam sodium (LY573636 sodium) as third-line treatment in patients with unresectable, metastatic non-small-cell lung cancer: a phase-II study

[3] Timothy Meier, et al. Mol Cancer Ther. Tasisulam sodium, an antitumor agent that inhibits mitotic progression and induces vascular normalization

[4] John M Kirkwood, et al. Cancer. A phase 2 study of tasisulam sodium (LY573636 sodium) as second-line treatment for patients with unresectable or metastatic melanoma

[5] George R Simon, et al. Cancer Chemother Pharmacol. A phase I study of tasisulam sodium (LY573636 sodium), a novel anticancer compound in patients with refractory solid tumors

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Keywords: Tasisulam sodium, LY 573636 sodium supplier, Apoptosis, inhibitors, activators

 
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