CX6258 Property

Boiling point:

697.8±55.0 °C(Predicted)

Density 

1.309±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in EtOH; ≥11.15 mg/mL in DMSO; ≥2.575 mg/mL in H2O with gentle warming

form 

solid

pka

11.38±0.20(Predicted)

color 

Yellow to orange

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.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

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

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

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

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

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

P405Store locked up.

P501Dispose of contents/container to..…

CX6258 Chemical Properties,Usage,Production

Uses

CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.

Biological Activity

pim kinases (provirus integration site for moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. this family of kinases is composed of three different isoforms (pim-1, pim-2, and pim-3). the simultaneous inhibition of pim-1, pim-2, and pim-3 kinases is emerging as a promising strategy for anticancer drug development. cx-6258 is a potent, selective, and orally efficacious pan-pim kinases inhibitor.

in vitro

cx-6258 exhibited in vitro synergy with chemotherapeutics. the antiproliferative activity of cx-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. cx-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1].

in vivo

cx-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia mv-4-11, and prostate adenocarcinoma pc3. the drug exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (tgi) and a 100 mg/kg dose producing 75% tgi. in addition, cx-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where pim kinases had been shown to play an important role [1].

target

Pim1

References

[1] haddach m, michaux j, schwaebe mk, et al. discovery of cx-6258. a potent, selective, and orally efficacious pan-pim kinases inhibitor. acs med chem lett. 2011;3(2):135-9.