| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B408030-1ml |
1ml |
现货  |
|
| 英文别名 | 4-(2-((1R,2R)-2-hydroxycyclohexylamino)benzo[d]thiazol-6-yloxy)-N-methylpicolinamide |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | BLZ945 |
| 生化机理 | BLZ945 是一种口服活性、强效和选择性 CSF-1R 抑制剂，IC50 为 1 nM，对最接近的受体酪氨酸激酶同源物的选择性大于 1000 倍。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 集落刺激因子 1 受体抑制剂；KIT 原癌基因受体酪氨酸激酶抑制剂；血小板衍生生长因子受体 beta 抑制剂 |
| 产品介绍 |
BLZ945 is a tumor-associated macrophage targeting the treatment of glioblastoma multiforme, a most common type of aggresive brain cancer. Information BLZ945 BLZ945 is an orally active, potent and selective CSF-1R inhibitor with IC50 of 1 nM, >1000-fold selective against its closest receptor tyrosine kinase homologs. In bone marrow-derived macrophages (BMDMs), BLZ945 specifically inhibits CSF-1-dependent proliferation with EC50 of 67nM, and decreases CSF-1R phosphorylation. BLZ945 blocks the reciprocal effects between macrophages and glioma cells on the survival, proliferation and/ or polarization of each other to promote tumorigenesis. In vivo In glioma-bearing mice, BLZ945 blocks tumor progression and significantly improves survival via CSF-1R inhibition. BLZ945 also inhibits orthotopic tumor growth of patient-derived proneural tumor spheres and cell lines in vivo. BLZ945 (200 mg/kg, p.o.) decreases the growth of malignant cells in both mouse mammary tumor virus-driven polyomavirus middle T antigen (MMTV-PyMT) model of mammary carcinogenesis and keratin 14-expressing human papillomavirus type 16 (K14-HPV-16) transgenic model of cervical carcinogenesis. cell lines：SCLC cell lines Concentrations：~6700 nM Incubation Time：96 hours Powder Purity:≥97% |
| ALogP | 3.201 |
|---|---|
| hba_count | 4 |
| HBD Count | 3 |
| Rotatable Bond | 5 |
| Canonical SMILES | CNC(=O)C1=NC=CC(=C1)OC2=CC3=C(C=C2)N=C(NC4CCCCC4O)S3 |
|---|---|
| 分子量 | 398.48 |
| Reaxy-Rn | 26002377 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26002377&ln= |
| DMSO(mg / mL) Max Solubility | 79 |
|---|---|
| DMSO(mM) Max Solubility | 198.25 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 26002377 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=26002377&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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