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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
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
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 415.11
Formula C11H6BrCl2NO3S2
CAS Number 519055-62-0
Purity >99%
Solubility DMSO 73 mg/mL
Storage at -20°C
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

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