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CX-4945(Silmitasertib)

Catalog No.: 52024
Cas No.: 1009820-21-6
Purity : 98% 
52024 - CX-4945(Silmitasertib) | CAS 1009820-21-6

Catalog number : 52024

CAS number : 1009820-21-6

分子式 : C19H12ClN3O2 

分子量 : 349.77 

Iupac 化学名称 : 5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylic acid 

Smile : ClC=1C=C(C=CC1)NC1=NC2=C(C3=CN=CC=C13)C=CC(=C2)C(=O)O

InChiKey : MUOKSQABCJCOPU-UHFFFAOYSA-N

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同义词CX-4945;Silmitasertib;CX4945;CX 4945 
英文同义词CX-4945;Silmitasertib;CX4945;CX 4945 
分子式C19H12ClN3O2 
分子量349.77 
外观yellow solid 
纯度98% 
可溶性5mg/ml in DMSO 
存储3 years -20ºCpowder 6 months-80ºCin solvent 
运输条件Shipped under ambient temperature 
SmileClC=1C=C(C=CC1)NC1=NC2=C(C3=CN=CC=C13)C=CC(=C2)C(=O)O
InChiKeyMUOKSQABCJCOPU-UHFFFAOYSA-N
InChiInChI=1S/C19H12ClN3O2/c20-12-2-1-3-13(9-12)22-18-15-6-7-21-10-16(15)14-5-4-11(19(24)25)8-17(14)23-18/h1-10H,(H,22,23)(H,24,25)
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1. Silmitasertib (CX-4945) is a potent and selective orally bioavailable small molecule inhibitor of Casein kinase II (CK2). The antiproliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. CX-4945 caused cell-cycle arrest and selectively induced apoptosis in cancer cells relative to normal cells. When administered orally in murine xenograft models, CX-4945 was well tolerated and demonstrated robust antitumor activity. Senhwa Biosciences is developing silmitasertib for the treatment of cholangiocarcinoma, other solid tumours, Castleman's disease (giant lymph node hyperplasia) and multiple myeloma. The compound was originally developed by Cylene Pharmaceuticals. Phase Ib/II development is underway in the US and South Korea for the treatment of cholangiocarcinoma, and development in the remaining indications is at the phase I stage. As at July 2016, no recent reports of development had been identified for phase-I development in Giant-lymph-node-hyperplasia in USA (PO, Capsule), phase-I development in Multiple-myeloma in USA (PO, Capsule), phase-I development in Solid-tumours (Late-stage disease) in USA (PO, Capsule).

2. Application 

In Vivo Use Guide 

Interim results of a phase I trial showed that silmitasertib was well-tolerated in patients with solid tumours. Thirteen such patients (3-4 patients per cohort, from four separate dose cohorts) received oral, twice-daily doses of silmitasertib for 21 consecutive days of a 4-week cycle. The trial design provided for administration of silmitasertib in successive dose cohorts at 90mg, 160mg, 300mg, 460mg, 700mg and 1000mg per dose. No adverse events of grade ≥3 were reported. No dose-limiting toxicities had been observed and the maximum tolerated dose was yet to be defined.

Route of Administration: Oral

In Vitro Use Guide 

Silmitasertib (CX-4945) exerts antiproliferative activity of in a panel of breast cancer cell lines with EC50 1.71-20.01 uM


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