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TAK-632 CAS NO.1228591-30-7
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≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
Keywords
- TAK-632
- TAK-632;N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide;TAK-0632;N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]
- 1228591-30-7
Quick Details
- ProName: TAK-632
- CasNo: 1228591-30-7
- Molecular Formula: C27H18F4N4O3S
- Appearance: close to white solid
- Application: CAS：1228591-30-7； TAK-632;N-[7-Cyano-...
- DeliveryTime: 2 months
- PackAge: 100g,500,1kg.....
- Port: shang hai
- ProductionCapacity: 1000 Gram/Month
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
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Our research team of scientists consists of western-trained Ph.D.s with experience and capabilities in drug R&D methodologies and medicinal chemistry.
Details
| TAK-632 |
| 生物活性 体外研究 体内研究 特征 |
| 中文名称: | TAK-632 |
| 中文同义词: | N-(7-CYANO-6-(4-FLUORO-3-(2-(3-(TRIFLUOROMETHYL)PHENYL)ACETAMIDO)PHENOXY)BENZO[D]THIAZOL-2-YL)CYCLOPROPANECARBOXAMIDE;N-[7-氰基-6-[4-氟-3-[[[3-(三氟甲基)苯基]乙酰基]氨基]苯氧基]-1,3-苯并噻唑-2-基]环丙烷甲酰胺;N-[7-氰基-6-[4-氟-3-[[[3-(三氟甲基)苯基]乙酰基]氨基]苯氧基]-1,3-苯并噻唑-2-基]环丙烷甲酰胺(TAK-632) |
| 英文名称: | TAK-632 |
| 英文同义词: | TAK-632;N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide;TAK-0632;N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide TAK632;TAK 632 N-[7-Cyano-6-[4-fluoro-3-[[[3-(trifluoromethyl)phenyl]acetyl]amino]phenoxy]-1,3-benzothiazol-2-yl]cyclopropanecarboxamide;TAK-632, >=98% |
| CAS号: | 1228591-30-7 |
| 分子式: | C27H18F4N4O3S |
| 分子量: | 554.5154328 |
| EINECS号: | -0 |
| 相关类别: | 小分子抑制剂;Inhibitors;小分子抑制剂，天然产物 |
| Mol文件: | 1228591-30-7.mol |
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| TAK-632 性质 |
| TAK-632 用途与合成方法 |
| 生物活性 | TAK-632是强效的泛Raf抑制剂，对B-Raf(wt)和C-Raf的IC50分别为8.3 nM and 1.4 nM， 对其他被测试的酶抑制效果较差或者没有效果。 |
| 体外研究 | TAK-632在黑色素瘤A375细胞系(BRAFV600E)中抑制MEK和ERK的磷酸化，其IC50分别为12 nM和16 nM。在人类黑色素瘤HMVII细胞系(NRASQ61K/BRAFG469V)中，TAK-632对pMEK和pERK显示出很强的抑制性，其IC50分别为49 nM和50 nM。并且，TAK-632在A375和HMVII系中还有很强的抗增殖活性，其GI50分别为66 nM 和200nM。TAK-632诱导RAF二聚化，同时由于从RAF中分离缓慢抑制了RAF的激酶活性。TAK-632和TAK-733联合用药对BRAF- 和NRAS-突变的黑色素瘤细胞起到协同的抗增殖作用。 |
| 体内研究 | TAK-632在老鼠和狗身上表现出优秀的口服利用率。在老鼠身上进行黑素瘤A375 (BRAFV600E)异种移植和人类黑素瘤HMVII (NRASQ61K/BRAFG469V)异种移植时，TAK-632 (3.9–24.1 mg/kg, p.o.) 表现出剂量依赖的抗癌效果，并且没有严重的体重减少。在NRAS-异变黑素瘤SK-MEL-2 异种移植模型中，TAK-632 (60 or 120 mg/kg, p.o.)也表现出强力的抗癌性，并且没有毒性。 |
| 特征 | Orally bioavailable, pan-raf inhibitor that targets both wild-type and mutant forms. |