PF-03814735 Property

Melting point:

181-183°C

Density 

1.443

storage temp. 

-20°C

solubility 

DMSO: soluble20mg/mL, clear

form 

powder

pka

15.02±0.46(Predicted)

color 

white to beige

Safety

WGK Germany 

3

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

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

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

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

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P362Take off contaminated clothing and wash before reuse.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

PF-03814735 Chemical Properties,Usage,Production

Description

The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC₅₀ values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC₅₀ values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT116, HL-60, A549, and H125 tumor cell lines with IC₅₀ values ranging from 42-150 nM and shows in vivo efficacy in an HCT116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.

Chemical Properties

Off-White Solid

Uses

The Aurora kinases are a family of serine/threonine kinases that are key regulators of mitosis and cytokinesis. PF-03814735 is a reversible inhibitor of both Aurora A and B kinases with IC50 values of 0.8 and 5 nM, respectively, in in vitro activity assays. PF-03814735 also inhibits the kinases FLT1, FAK, TrkA, Met, and FGFR1 with IC50 values of 10, 22, 30, 100, and 100 nM, respectively. PF-03814735 inhibits cell proliferation of HCT-116, HL-60, A549, and H125 tumor cell lines with IC50 values ranging from 42-150 nM and shows in vivo efficacy in an HCT-116 tumor xenograft mouse model. PF-03814735 has been shown to be particularly sensitive towards inhibiting the growth of small cell lung cancer cell lines and other tumors driven by the Myc family genes.[Cayman Chemical]

Uses

PF 03814735 is an orally bioavailable small molecule aurora kinase inhibitor that plays a key role in the regulation of mitosis. PF 03814735 is a anticancer agent used for cancer therapy.

storage

-20°C

References

[1] jani jp, arcari j, bernardo v, bhattacharya sk, briere d, cohen bd, coleman k, christensen jg, emerson eo, jakowski a, hook k, los g, moyer jd, pruimboom-brees i, pustilnik l, rossi am, steyn sj, su c, tsaparikos k, wishka d, yoon k, jakubczak jl. pf-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy. mol cancer ther. 2010 apr;9(4):883-94.