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)

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.