LDK378

Ceritinib (LDK378) is a selective, orally bioavailable, and ATP-competitive ALK tyrosine kinase inhibitor with an IC50 of 200 pM. Ceritinib (LDK378) also inhibits IGF-1R, InsR, and STK22D with IC50 values of 8, 7, and 23 nM, respectively. Ceritinib (LDK378) shows great antitumor potency.


Cat. No.: EX-A187	Purity: >98%

	Chemical structure of LDK378

For research only, Do not use for Human!

Size	Unit Price (US$)	Stock	Quantity	Order
10g	293	in_stock

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Synonyms	Ceritinib
CAS No.	1032900-25-6
Purity	>98%
Formula	C28H36ClN5O3S
Mol Weight	558.135
Color	white to off-white
State	solid powder
Solubility	Soluble in DMSO
Shelf Life	>2 years if stored properly
Storage	Powder -20℃ 2 years; In solvent -20℃ 1 month;
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[1]. Marsilje TH, et al. 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 clinical trials. J Med Chem. 2013 Jul 25;56(14):5675-90. [2]. Chen J, et al. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4. [3]. Tucker ER, et al. Immunoassays for the quantification of ALK and phosphorylated ALK support the evaluation of on-target ALK inhibitors in neuroblastoma. Mol Oncol. 2017 Aug;11(8):996-1006. [4]. Rothschild SI. Ceritinib-a second-generation ALK inhibitor overcoming resistance in ALK-rearranged non-small celllung cancer. Transl Lung Cancer Res. 2014 Dec;3(6):379-81.
CoA	CoA of LDK378

Smiles:	CC(C)OC1=CC(C2CCNCC2)=C(C)C=C1NC1=NC=C(Cl)C(NC2=CC=CC=C2S(=O)(=O)C(C)C)=N1


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