BMS-911543 Property

storage temp. 

under inert gas (nitrogen or Argon) at 2–8 °C

solubility 

≥43.3 mg/mL in DMSO with gentle warming; insoluble in H2O; ≥9.8 mg/mL in EtOH with gentle warming and ultrasonic

form 

Powder

color 

White to light yellow

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..…

BMS-911543 Chemical Properties,Usage,Production

Uses

BMS 911543 is a functionally selective small molecule inhibitor of JAK2 and have been developed as a treatment for leukemia.

Biological Activity

bms-911543 is a selective small-molecule inhibitor of jak2 with ic50 value of 1.1nm [1].bms-911543 is a reversible pyrrolopyridine atp-competitive jak2 inhibitor with a high selectivity. in the in vitro assay using human recombinant jak enzyme, bms-911543 displays an ic50 value of 1.1nm against jak2 and the ki value is 0.48nm. the inhibition activity and affinity against jak2 are both much higher than those against jak1 and jak3. besides that, bms-911543 also has efficacy against other kinases, such as lyn and the c-fms receptor tyrosine kinase. in jak-dependent cells such as set2 or ba/f3, the treatment of bms-911543 causes an anti-proliferative effect with ic50 values of 60 and 70nm, respectively. the cell lines depending on other jak family members do not show significant anti-proliferative response to bms-911543. the colony growth assays prove that bms-911543 can suppress the growth of mpn patient-derived cells and is more potent in the jak2v617f pathway compared with the jak2wt pathway. bms-911543 is also found to be potent in vivo in both the jak2wt pathway and the jak2v617f pathway through suppressing pstat5 induction [1].

target

JAK2

References

[1] purandare av, mcdevitt tm, wan h, you d, penhallow b, han x, vuppugalla r, zhang y, ruepp su, trainor gl, lombardo l, pedicord d, gottardis mm, ross-macdonald p, de silva h, hosbach j, emanuel sl, blat y, fitzpatrick e, taylor tl, mcintyre kw, michaud e, mulligan c, lee fy, woolfson a, lasho tl, pardanani a, tefferi a, lorenzi mv. characterization of bms-911543, a functionally selective small-molecule inhibitor of jak2. leukemia. 2012 feb;26(2):280-8.