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LY573636 (Tasisulam)

Cat. No. M2551
LY573636 (Tasisulam) Structure
Synonym:

Tasisulam

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 35  USD35 In stock
10mg USD 60  USD60 In stock
50mg USD 210  USD210 In stock
100mg USD 320  USD320 In stock
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Quality Control & Documentation
Biological Activity

LY573636 is a novel anticancer agent that induces apoptosis through the intrinsic pathway and has antiangiogenic activity in preclinical models. LY573636 demonstrated activity across a broad range of tumors, including melanoma. LY573636 causes growth arrest and apoptosis of a variety of human solid tumors in vitro and in vivo. LY573636 administered at a targeted C(max) of 420 μg/mL on Day 1 of 21-day cycles demonstrated activity and tolerable toxicity as second-line treatment in malignant melanoma. LY573636 is selectively toxic towards tumor cells over their normal counterparts.

Customer Product Validations & Biological Datas
Source Mol Cancer Ther (2011). Figure 1. LY 573636
Method FACS analysis
Cell Lines Calu-6 and A-375 cell
Concentrations from 200 mmol/L to approximately 200 nmol/L
Incubation Time 72 hours
Results Fluorescence-activated cell sorting (FACS) analysis of Calu-6 and A-375 cell lines showed that tasisulam induced a concentration-dependent increase in 4N DNA
Chemical Information
Molecular Weight 415.11
Formula C11H6BrCl2NO3S2
CAS Number 519055-62-0
Solubility (25°C) DMSO 73 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] Kirkwood JM, et al. Cancer. A phase 2 study of tasisulam sodium (LY573636 sodium) as second-line treatment for patients with unresectable or metastatic melanoma.

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Keywords: LY573636 (Tasisulam), Tasisulam supplier, Caspase, inhibitors, activators


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