TP0903 Property

Melting point:

>198°C (dec.)

Boiling point:

664.7±65.0 °C(Predicted)

Density 

1.347±0.06 g/cm3(Predicted)

storage temp. 

Hygroscopic, -20°C Freezer, Under inert atmosphere

solubility 

Chloroform (Slightly), Methanol (Slightly)

pka

7.60±0.10(Predicted)

form 

Solid

color 

Off-White to Light Yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

TP0903 Chemical Properties,Usage,Production

Uses

TP-0903 is an AXL kinase inhibitor.

Biological Activity

axl and other tam family members are known to be involved in maintaining the mesenchymal phenotype in cancer cells. mesenchymal cells have increased invasion and migratory properties, enhanced cell survival in stressed environments, as well as increased resistance to targeted therapies. tp-0903 is a potent anti-cancer agent targeting the axl receptor tyrosine kinase.

in vitro

on the basis of the potency of tp-0903 in biochemical assays, its activity in cell-based studies was evaluated. tp-0903 showed extremely potent activity in cell viability assays against the pancreatic cancer cell line psn-1. more importantly, tp-0903 was evaluated for its ability to block gas6-mediated activation of axl in pancreatic cancer cells. psn-1 cells were serum-starved and then stimulated with gas6 in the presence of various concentrations of tp-0903 [1].

in vivo

tp-0903 restores sensitivity to erlotinib in cell-based and preclinical animal models of cancer by reversing the mesenchymal phenotype driving resistance [2].

IC 50

0.027 μm against axl

References

[1] mollard a, warner sl, call lt, wade ml, bearss jj, verma a, sharma s, vankayalapati h, bearss dj. design, synthesis and biological evaluation of a series of novel axl kinase inhibitors. acs med chem lett. 2011 dec 8;2(12):907-912.
[2] toleropharmaceuticals, inc–tp-0903. http://www.toleropharmaceuticals.com/tp-0903.html.