KRC-108
CAS 1146944-35-5 MFCD246944355
化学结构图
SMILES: Nc1ncc(-c2cnn(C3CCNCC3)c2)cc1-c1nc2ccccc2o1
化学属性
| Mol. Weight | 433.33 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | KRC-108 |
|---|---|
| Formula | C20H20N6O-2HCl or C20H22Cl2N6O |
| Synonym | KRC108; KRC 108; KRC-108 |
| IUPAC Name | 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine |
| InChIKey | NLOGXCAMKYLWJP-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H20N6O/c21-19-16(20-25-17-3-1-2-4-18(17)27-20)9-13(10-23-19)14-11-24-26(12-14)15-5-7-22-8-6-15/h1-4,9-12,15,22H,5-8H2,(H2,21,23) |
| Canonical SMILES | NC1=NC=C(C2=CN(C3CCNCC3)N=C2)C=C1C4=NC5=CC=CC=C5O4 |
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产品应用
- KRC-108 is a multiple kinase inhibitor. KRC-108 is a potent inhibitor of Ron, Flt3 and TrkA as well as c-Met. KRC-108 inhibited oncogenic c-Met M1250T and Y1230D more strongly than wild type c-Met. The anti-proliferative activity of KRC-108 was measured by performing a cytotoxicity assay on a panel of cancer cell lines. The GI(50) values (i.e., 50% inhibition of cell growth) for KRC-108 ranged from 0.01 to 4.22 μM for these cancer cell lines. KRC-108 was also effective for the inhibition of tumor growth in human HT29 colorectal cancer and NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice. This molecule should serve as a useful lead for inhibitors targeting kinases and may lead to new therapeutics for the treatment of cancer. (source: Invest New Drugs. 2012 Apr;30(2):518-23. doi: 10.1007/s10637-010-9584-2. Epub 2010 Nov 16. ).
