PKI-402 Property

Boiling point:

670.6±55.0 °C(Predicted)

Density 

1.43

storage temp. 

Store at -20°C

solubility 

insoluble in EtOH; insoluble in H2O; ≥14.28 mg/mL in DMSO

form 

solid

pka

13.80±0.70(Predicted)

color 

White to off-white

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P273Avoid release to the environment.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P391Collect spillage. Hazardous to the aquatic environment

P501Dispose of contents/container to..…

PKI-402 Chemical Properties,Usage,Production

Uses

A selective, reversible and ATP-competitive Class I PI3K inhibitor. PI3Kα, IC50=1 nM; PI3Kβ, IC50=7 nM; PI3Kγ, IC50=16 nM; PI3Kδ, IC50=14 nM.

Uses

PKI 402 is a potent pan-PI3K/mTOR dual inhibitor and a potential antitumor drug.

Biological Activity

pki-402 is a selective, equipotent and atp-competitive class i pi3k inhibitor (ic50= 1 nm, 7 nm, 16 nm and 14 nm for pi3kα, pi3kβ, pi3kγ and pi3kδ, respectively.)pi3k (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. it plays a key role in pi3k/akt/mtor pathway.in multiple human cancer cell lines (e.g. breast, brain, pancreas and nscl), pki-402 inhibited growth of cancer cells, and attenuated phosphorylation of effector of pi3k and mtor. in mda-mb-361, 30 nm pki-402 caused cleaved of the apoptosis marker—parp.in mda-mb-361 mouse tumor xenograft models, administration of 100 mg/kg of pki-402 daily for 5 days decreased the initial tumor volume from 260 mm3 to 129 mm3 and inhibited tumor regrowth for 70 days, single dose of pki-402 blocked phosphorylation of akt and led to cleaved parp.1. mallon r, hollander i, feldberg l et al. antitumor efficacy profile of pki-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. mol cancer ther. 2010 apr;9(4):976-84.

target

PI3Kα