货号:A107516 同义名: TAK-580;MLN2480
Tovorafenib (TAK-580, MLN 2480) 是一种可口服的,具有选择性的广谱的 Raf 抑制剂。Tovorafenib (TAK-580, MLN 2480) 通过抵消 TAK-733 触发的 MEK 反馈激活,导致 MAPK 通路的协调抑制。
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产品名称 | A-raf ↓ ↑ | B-Raf ↓ ↑ | C-Raf/Raf-1 ↓ ↑ | Raf ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Encorafenib | ✔ | 99%+ | |||||||||||||||||
GDC-0879 |
++++
B-Raf, IC50: 0.13 nM |
99%+ | |||||||||||||||||
SB-590885 |
++++
B-Raf, Ki: 0.16 nM |
99%+ | |||||||||||||||||
RAF265 | 99%+ | ||||||||||||||||||
Dabrafenib |
++++
B-Raf, IC50: 5.2 nM B-Raf (V600E), IC50: 0.7 nM |
+++
C-Raf, IC50: 6.3 nM |
98% | ||||||||||||||||
Lifirafenib |
++++
WT A-RAF, IC50: 1 nM |
++
BRAF WT, IC50: 32 nM BRAF(V600E), IC50: 23 nM |
+++
C-RAF (Y340/341D), IC50: 7 nM |
EGFR | 98% | ||||||||||||||
ZM 336372 |
+
C-Raf, IC50: 70 nM |
99%+ | |||||||||||||||||
NVP-BHG 712 |
+
C-Raf, IC50: 0.395 μM |
99%+ | |||||||||||||||||
CCT196969 |
+
BRAF, IC50: 0.1 μM |
++
CRAF, IC50: 0.01 μM |
Src | 98% | |||||||||||||||
Vemurafenib |
++
B-Raf, IC50: 100 nM B-Raf (V600E), IC50: 31 nM |
+
C-Raf, IC50: 48 nM |
98+% | ||||||||||||||||
PLX4720 |
++
B-Raf, IC50: 160 nM B-Raf (V600E), IC50: 13 nM |
+++
C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM |
BRK | 99+% | |||||||||||||||
GW 5074 |
+++
C-Raf, IC50: 9 nM |
99%+ | |||||||||||||||||
Avutometinib |
+++
BRAF, IC50: 19 nM BRAF V600E, IC50: 8.2 nM |
+
CRAF, IC50: 56 nM |
98% | ||||||||||||||||
LY3009120 |
++++
BRAF WT, IC50: 15 nM BRAF(V600E), IC50: 5.8 nM |
++++
C-Raf, IC50: 4.3 nM |
99%+ | ||||||||||||||||
Agerafenib |
++
B-Raf (V600E), Kd: 14 nM B-Raf, Kd: 36 nM |
+
C-Raf, Kd: 39 nM |
RET | 99%+ | |||||||||||||||
TAK-632 |
+++
B-Raf, IC50: 8.3 nM |
++++
C-Raf, IC50: 1.4 nM |
99%+ | ||||||||||||||||
AZ 628 |
+
B-Raf, IC50: 105 nM B-Raf (V600E), IC50: 34 nM |
++
C-Raf-1, IC50: 29 nM |
99% | ||||||||||||||||
PLX7904 | ✔ | 98+% | |||||||||||||||||
Sorafenib |
++
B-Raf, IC50: 22 nM B-Raf (V599E), IC50: 38 nM |
++++
Raf-1, IC50: 6 nM |
++++
Raf-1, IC50: 6 nM |
99% | |||||||||||||||
Tovorafenib | ✔ | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Tovorafenib (TAK-580, MLN 2480) acts by counteracting the feedback activation of MEK triggered by TAK-733, resulting in more coordinated inhibition of the MAPK pathway [1]. |
体内研究 | Tovorafenib (TAK-580, MLN 2480) suppresses MAPK pathway signaling in preclinical cancer models harboring BRAF mutations and certain RAS mutations at concentrations tolerated in vivo. TAK-580 (MLN 2480) demonstrates heightened efficacy in BRAF mutant melanoma models, and it also exhibits activity as a single agent in select RAS mutant models. Combination therapy involving MLN2480 with TAK-733 impedes the growth of a wider spectrum of RAS mutant tumor models compared to TAK-580 (MLN 2480) alone, including primary human tumor xenograft models of melanoma and CRC [1]. |
体外研究 | Tovorafenib (TAK-580, MLN 2480) acts by counteracting the feedback activation of MEK triggered by TAK-733, resulting in more coordinated inhibition of the MAPK pathway [1]. |
Dose | Mice: 12.5 mg/kg[2] (p.o.), 30 mg/kg[3] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.98mL 0.40mL 0.20mL |
9.88mL 1.98mL 0.99mL |
19.75mL 3.95mL 1.98mL |
CAS号 | 1096708-71-2 |
分子式 | C17H12Cl2F3N7O2S |
分子量 | 506.289 |
别名 | TAK-580;MLN2480;BUB 024;DAY-101;BSK1369;AMG-2112819;BIIB-024 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 105 mg/mL(207.39 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |