BLZ945
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- CAS号:
- 953769-46-5
- 英文名:
- 4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide
- 英文别名:
- BLZ945;106245;CS-1735;4-((2-(((1R;Sotuletinib;BLZ-945 >=95%;BLZ-945;BLZ 945;Sotuletinib (BLZ945);2R)-2-hydroxycyclohexyl)imino)-2;3-dihydrobenzo[d]thiazol-6-yl)oxy)-N-methylpicolinamide
- 中文名:
- BLZ945
- 中文别名:
- 化合物BLZ945;CSF-1R抑制剂(BLZ945);PERFEMIKER]BLZ945,99%;2R)-2-羟基环己基)氨基)苯并[D]噻唑-6-基)氧基)-N-甲基吡啶酰胺;4-((2-(((1R,2R)-2-羟基环己基)氨基)苯并[D]噻唑-6-基)氧基)-N-甲基吡啶酰胺;4-[[2-[[(1R,2R)-2-羟基环己基]氨基]-6-苯并噻唑基]氧基]-N-甲基吡啶-2-甲酰胺
- CBNumber:
- CB42706230
- 分子式:
- C20H22N4O3S
- 分子量:
- 398.48
- MOL File:
- 953769-46-5.mol
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BLZ945化学性质
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密度:
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1.377±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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insoluble in EtOH; insoluble in H2O; ≥19.9 mg/mL in DMSO
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形态:
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solid
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酸度系数(pKa):
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13.92±0.46(Predicted)
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颜色:
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Pale yellow
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BLZ945性质、用途与生产工艺
BLZ945是一种具有口服活性的,有效的选择性 CSF-1R抑制剂,IC50为1 nM,比其最接近的受体酪氨酸激酶同系物高出1000多倍的选择性。
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 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.
BLZ945是一种具有口服活性的,有效的选择性 CSF-1R抑制剂,IC50为1 nM,比其最接近的受体酪氨酸激酶同系物高出1000多倍的选择性。
Target | Value |
CSF-1R
(Cell-free assay)
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1 nM
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在骨髓衍生的巨噬细胞(BMDMs)中,BLZ945特异性抑制CSF-1依赖性增殖,EC50 为67nM,并减少CSF-1R磷酸化。BLZ945阻断巨噬细胞和胶质瘤细胞在存活,增殖和/或偏振中的相互作用,从而抑制其促肿瘤发生。
在负荷神经胶质瘤的小鼠体内,BLZ945阻断肿瘤发展,并通过CSF-1R抑制显著提高存活率。BLZ945也会抑制来源于患者的原神经肿瘤球和细胞系在体内的正位肿瘤生长。在小鼠乳腺肿瘤病毒驱动的致乳腺癌的多瘤病毒中间T抗原(MMTV-PyMT)模型,和角蛋白14表达的致宫颈癌变的16型人乳头瘤病毒(K14-HPV-16)转基因模型中,BLZ945 (200 mg/kg, p.o.)减少恶性细胞的生长。
BLZ945
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/08/19 | HY-12768 | Sotuletinib | | 1 mg | 340元 |
2024/08/19 | HY-12768 | BLZ945 Sotuletinib | 953769-46-5 | 5 mg | 750元 |
953769-46-5, BLZ945 相关搜索:
- API
- Inhibitors
- 合成有机化合物配体
- 药物活性分子
- 细胞生物学试剂
- 抑制剂
- 小分子抑制剂,天然产物
- PERFEMIKER]BLZ945,99%
- 4-((2-(((1R,2R)-2-羟基环己基)氨基)苯并[D]噻唑-6-基)氧基)-N-甲基吡啶酰胺
- 4-[[2-[[(1R,2R)-2-羟基环己基]氨基]-6-苯并噻唑基]氧基]-N-甲基吡啶-2-甲酰胺
- 2R)-2-羟基环己基)氨基)苯并[D]噻唑-6-基)氧基)-N-甲基吡啶酰胺
- 化合物BLZ945
- CSF-1R抑制剂(BLZ945)
- 953769-46-5
- Sotuletinib (BLZ945)
- CSF1R,CSF-1R,CSF-1 receptor,inhibit,c-Fms,Inhibitor,colony stimulating factor 1 receptor,BLZ 945,Sotuletinib,BLZ-945
- Sotuletinib
- BLZ945
- 4-[[2-[[(1R,2R)-2-Hydroxycyclohexyl]amino]-6-benzothiazolyl]oxy]-N-methylpyridine-2-carboxamide
- 4-((2-(((1R
- 3-dihydrobenzo[d]thiazol-6-yl)oxy)-N-methylpicolinamide
- 2R)-2-hydroxycyclohexyl)imino)-2
- 4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide USP/EP/BP
- 2-Pyridinecarboxamide, 4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-6-benzothiazolyl]oxy]-N-methyl-
- 4-[(2-{[(1R,2R)-2-Hydroxycyclohexyl]amino}-1,3-benzothiazol-6-yl)oxy]-N-methyl-2-pyridinecarboxamide
- CS-1735
- BLZ-945;BLZ 945
- 106245
- 4-[[2-[[(1R,2R)-2-hydroxycyclohexyl]amino]-1,3-benzothiazol-6-yl]oxy]-N-methylpyridine-2-carboxamide
- BLZ-945 >=95%
- 4-[[2-[[(1R,2R)-2-Hydroxycyclohexyl]amino]-6-benzothiazolyl]oxy]-N-methyl-2-pyridinecarboxamide
- 4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide
BLZ945
- 4-((2-(((1R,2R)-2-hydroxycyclohexyl)aMino)benzo[d]thiazol-6-yl)oxy)-N-MethylpicolinaMide