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HomeProduct name listLDK-378 dihydrochloride

LDK-378 dihydrochloride

LDK-378 dihydrochloride Structural

What is LDK-378 dihydrochloride?

Biological Activity

ldk378 is a highly potent inhibitor of anaplastic lymphoma kinase (alk), which is a receptor tyrosine kinase belonging to the superfamily of insulin receptor, with half maximal inhibitory concentration ic50 of 200 pm. ldk378 also exhibits modest to high inhibition against a panel of other kinases, in which only three kinases with ic50 below 100 nm includes igf-1r (8 nm), insr (7 nm) and stk22d (23 nm). in previous studies, ldk378 has been found to inhibit the proliferation of ba/f3 cells transfected with the npm-alk fusion gene and karpas 299 human non-hodgkin’s ki-positivr large cell lymphoma harboring the npm-alk fusion gene with ic50 of 22.8 nm and 26 nm.

References

[1]chen j, jiang c, wang s. ldk378: a promising anaplastic lymphoma kinase (alk) inhibitor. j med chem. 2013 jul 25;56(14):5673-4. doi: 10.1021/jm401005u. epub 2013 jul 9.
[2]marsilje th, pei w, chen b, lu w, uno t, jin y, jiang t, kim s, li n, warmuth m, sarkisova y, sun f, steffy a, pferdekamper ac, li ag, joseph sb, kim y, liu b, tuntland t, cui x, gray ns, steensma r, wan y, jiang j, chopiuk g, li j, gordon wp, richmond w, johnson k, chang j, groessl t, he yq, phimister a, aycinena a, lee cc, bursulaya b, karanewsky ds, seidel hm, harris jl, michellys py. synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (alk) inhibitor 5-chloro-n2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-n4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (ldk378) currently in phase 1 and phase 2

Properties of LDK-378 dihydrochloride

storage temp.  Store at -20°C
solubility  ≥12.38 mg/mL in EtOH with ultrasonic; ≥13.7 mg/mL in H2O; ≥29.65 mg/mL in DMSO
form  Powder
color  Light yellow to yellow

Safety information for LDK-378 dihydrochloride

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
H315:Skin corrosion/irritation
H319:Serious eye damage/eye irritation
H335:Specific target organ toxicity, single exposure;Respiratory tract irritation
Precautionary Statement Codes P261:Avoid breathing dust/fume/gas/mist/vapours/spray.
P301+P312:IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352:IF ON SKIN: wash with plenty of soap and water.
P304+P340:IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for LDK-378 dihydrochloride

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