产品名称

英文名称：CX-4945 (Silmitasertib)

同义词

Silmitasertib、1009820-21-6、CX-4945、5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid、CX 4945、CX-4945 (Silmitasertib)、CX4945、Silmitasertib [INN]、Cx-4945 free acid、UNII-C6RWP0N0L2、CX4945 (Silmitasertib)、C6RWP0N0L2、5-(3-chlorophenylamino)

产品性质

CAS编号：1009820-21-6

分子式：C19H12ClN3O2

分子量：349.77

PubChem编号：24748573

英文别名：Silmitasertib|1009820-21-6|CX-4945|5-((3-Chlorophenyl)amino)benzo[c][2,6]naphthyridine-8-carboxylic acid|CX 4945|CX-4945 (Silmitasertib)|CX4945|Silmitasertib [INN]|Cx-4945 free acid|UNII-C6RWP0N0L2|CX4945 (Silmitasertib)|C6RWP0N0L2|5-(3-chlorophenylamino)

规格或纯度：≥98%

英文名称：CX-4945 (Silmitasertib)

生化机理：CX-4945 (Silmitasertib) is an ATP-competitive CK2 protein kinase inhibitor with a Ki and an IC50 of 0.38 and 1 nM for recombinant human CK2α, respectively. CX-4945 has broad-spectrum anti-proliferative activity in multiple cancer cell lines. The anti-proliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. Attenuation of PI3K/Akt signaling by CX-4945 was evidenced by dephosphorylation of Akt on the CK2-specific S129 site and the canonical S473 and T308 regulatory sites. CX-4945 suppresses Akt signaling and inhibits proliferation of HUVEC Cells. CX-4945 causes cell-cycle arrest and selectively induced apoptosis in certain cancer cells. In models of angiogenesis, CX-4945 inhibited human umbilical vein endothelial cell migration, tube formation, and blocked CK2-dependent hypoxia-induced factor 1 alpha (HIF-1α) transcription in cancer cells. Collectively, CX-4945 inhibits pro-angiogenic CK2 signaling in vitro and in vivo.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：卖完停产，不再备货

产品介绍：CX-4945 (Silmitasertib)是有效的，选择性CK2(casein kinase 2)抑制剂，无细胞试验中IC50为1 nM,对 Flt3, Pim1 和 CDK1作用效果稍弱(细胞试验中没有活性)。An ATP-competitive CK2 protein kinase inhibitor.CX-4945 (Silmitasertib) is a potent and selective inhibitor of CK2 (casein kinase 2) with IC50 of 1 nM in a cell-free assay, less potent to Flt3, Pim1 and CDK1 (inactive in cell-based assay).An ATP-competitive CK2 protein kinase inhibitor.

ALogP：4.4

IUPAC Name：5-(3-chloroanilino)benzo[c][2,6]naphthyridine-8-carboxylic acid

INCHI：InChI=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)

InChi Key：MUOKSQABCJCOPU-UHFFFAOYSA-N

Canonical SMILES：C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4

Isomeric SMILES：C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4

PubChem CID：24748573

ChEMBL Ligand：CHEMBL1230165

CAS Registry No.：1009820-21-6

RCSB PDB Ligand：3NG

溶解性：Soluble in water (<1.2 mg/ml), DMSO (≥65 mg/ml), and ethanol (<1.2 mg/ml).

产品包装