| Identification | Back Directory | [Name]
LDK-378 dihydrochloride | [CAS]
1380575-43-8 | [Synonyms]
LDK378 2Hcl
5-Chloro-N4-[
Ceritinib 2hcl
Ceritinib diHCl
Ceritinib intermediate
Ceritinib Hydrochloride
LDK 378 dihydrochloride
LDK-378 dihydrochloride
LDK378 2HCl (Ceritinib)
LDK378 (dihydrochloride)
Ceritinib dihydrochloride
LDK378 (Ceritinib) dihydrochloride
LDK378 dihydrochloride, Ceritinib dihydrochloride
CERITINIB DIHYDROCHLORIDE (LDK378 DIHYDROCHLORIDE)
LDK 378 DIHYDROCHLORIDE; LDK-378 DIHYDROCHLORIDE; CERITINIB DIHYDROCHLORIDE
5-chloro-N2-(2-isopropoxy-5-Methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyriMidine-2,4-diaMine hydrochloride
5-CHLORO-N2-(2-ISOPROPOXY-5-METHYL-4-(PIPERIDIN-4-YL)PHENYL)-N4-(2-(ISOPROPYLSULFONYL)PHENYL)PYRIMIDINE-2,4-DIAMINE DIHYDROCHLORIDE
5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine,dihydrochloride
5-Chloro-N4-[2-[(1-methylethyl)sulfonyl]phenyl]-N2-[5-methyl-2-(1-methylethoxy)-4-(4-piperidinyl)phenyl]-2,4-pyrimidinediamine hydrochloride (1:2) | [Molecular Formula]
C28H37Cl2N5O3S | [MDL Number]
MFCD26142928 | [MOL File]
1380575-43-8.mol | [Molecular Weight]
594.596 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 |
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