021-51111890
购物车（0）
sales@molnova.cn
TAK-659
CAS No. 1312691-33-0
TAK-659 ( Mivavotinib | TAK 659 | TAK659 )
产品货号. M11256 CAS No. 1312691-33-0
TAK-659（TAK659，Mivavotinib）是一种有效的、选择性的、口服的 SYK 抑制剂，IC50 为 3.2 nM。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ￥9477 | 有现货 |
|
| 50MG | ￥19278 | 有现货 |
|
| 100MG | ￥25110 | 有现货 |
|
| 200MG | 获取报价 | 有现货 |
|
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
-
产品名称TAK-659
-
注意事项本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
-
产品简述TAK-659（TAK659，Mivavotinib）是一种有效的、选择性的、口服的 SYK 抑制剂，IC50 为 3.2 nM。
-
产品描述TAK-659 (TAK659, Mivavotinib) is a potent, selective and orally available SYK inhibitor with IC50 of 3.2 nM; displays 36, 42 and 23-fold selectivity over JAK3, ZAP70 and VEGFR2, respectively; also potently inhibits FLT-3; inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines, demonstrates potent tumor growth inhibition in the FLT3-dependent MV4-11 xenograft models.Blood Cancer Phase 2 Clinical.
-
体外实验TAK-659 inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines.TAK-659 (5 μM; 1-24 hours) induces Casp3 activation in the LMP2A/MYC cells which was readily apparent at 4 h and reached maximum levels at 8 h of treatment.TAK-659 (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells.Apoptosis Analysis Cell Line:LMP2A/MYC cells Concentration:5 μM Incubation Time: 1 hour, 2 hours, 4 hours, 8 hours, 24 hoursResult:Induced apoptosis in LMP2A/MYC lymphoma cells.Western Blot Analysis Cell Line:Ramos cells Concentration:0.01 μM,0.1 μM,1 μM,10 μM Incubation Time:1 hour Result:Enhanced expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 in stimulated Ramos cells.
-
体内实验TAK-659 (100 mg/kg/day; p.o.; for 10 days) treatment totally abrogates splenomegaly and tumor development in LMP2A/MYC mice in both pretumor and tumor cell transfer experiments. TAK-659 treatment kills tumor cells, but not host cells within the spleen and tumors.TAK-659 treatment abrogates metastasis of tumor cells into bone marrow. Animal Model:LMP2A/MYC double transgenic mice Dosage:100 mg/kg/day Administration:Oral gavage; for 10 days Result:Inhibited LMP2A-induced tumor cell survival in vivo.
-
同义词Mivavotinib | TAK 659 | TAK659
-
通路Angiogenesis
-
靶点Syk
-
受体Syk
-
研究领域Cancer
-
适应症Blood cancer
化学信息
-
CAS Number1312691-33-0
-
分子量344.394
-
分子式C17H21FN6O
-
纯度>98% (HPLC)
-
溶解度——
-
SMILESCN1C=C(C=N1)C2=NC(=C(C3=C2C(=O)NC3)F)NC4CCCCC4N
-
化学全称6-(((1R,2S)-2-aminocyclohexyl)amino)-7-fluoro-4-(1-methyl-1H-pyrazol-4-yl)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one
运输与储存
-
储存条件(-20℃)
-
运输条件With Ice Pack
-
稳定性≥ 2 years
参考文献
1. Lam B, et al. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5947-5950.
2. Purroy N, et al. Oncotarget. 2017 Jan 3;8(1):742-756.
3. Liu D, et al. J Hematol Oncol. 2017 Jul 28;10(1):145.
产品手册
关联产品
-
TC-S 7003
Lck Inhibitor 是一种有效的口服活性淋巴细胞特异性激酶 (Lck) 抑制剂，对 Lck，Lyn，Src 和 Syk 激酶的 IC50 分别为 7、2.1、4.2 和 200 nM。与 MAPK，CDK 和 RSK 家族代表相比，Lck Inhibitor 对 Lck 的选择性高出 1000 倍以上。Lck Inhibitor 抑制 T 细胞增殖和关节炎模型。
-
R406 free base
R406（游离碱）是一种有效的 Syk 抑制剂，在无细胞测定中 IC50 为 41 nM。
-
MNS
MNS 是一种酪氨酸激酶抑制剂，抑制 Syk、Src、p97，IC50 分别为 2.5 μM、29.3 μM 和 1.7 μM。
