B-Raf inhibitor, a pyrazine and pyrrolo[2,3-b]pyridine derivative, is useful in the treatment of cancer and proliferative diseases.
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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(V600E), IC50: 23 nM BRAF WT, IC50: 32 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(V600E), IC50: 5.8 nM BRAF WT, IC50: 15 nM |
++++
C-Raf, IC50: 4.3 nM |
99%+ | ||||||||||||||||
Agerafenib |
++
B-Raf, Kd: 36 nM B-Raf (V600E), Kd: 14 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 (V599E), IC50: 38 nM B-Raf, IC50: 22 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。 |
描述 | B-Raf inhibitor, a pyrazine and pyrrolo[2,3-b]pyridine derivative, is useful in the treatment of cancer and proliferative diseases. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03181100 | Malignant Neoplasms of Thyroid... 展开 >> and Other Endocrine Glands Anaplastic Thyroid Carcinoma Poorly Differentiated Thyroid Cancer 收起 << | Phase 2 | Recruiting | July 2023 | United States, Texas ... 展开 >> University of Texas MD Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Clinical Research Operations mcabani@mdanderson.org Contact mcabani@mdanderson.org 收起 << |
NCT01978236 | Melanoma and Brain Metastases | Phase 2 | Terminated(This study was term... 展开 >>inated due to the limited enrollment.) 收起 << | - | United States, Pennsylvania ... 展开 >> GSK Investigational Site Pittsburgh, Pennsylvania, United States, 15232 United States, Texas GSK Investigational Site Houston, Texas, United States, 77030 Australia, New South Wales GSK Investigational Site North Sydney, New South Wales, Australia, 2060 收起 << |
NCT01738451 | Cancer | Phase 1 | Completed | - | United States, Arizona ... 展开 >> GSK Investigational Site Scottsdale, Arizona, United States, 85259 United States, Tennessee GSK Investigational Site Memphis, Tennessee, United States, 38120 GSK Investigational Site Nashville, Tennessee, United States, 37203 United States, Texas GSK Investigational Site San Antonio, Texas, United States, 78229 United States, Utah GSK Investigational Site Salt Lake City, Utah, United States, 84112-5550 Australia, Victoria GSK Investigational Site Heidelberg, Victoria, Australia, 3084 GSK Investigational Site Melbourne, Victoria, Australia, 3004 United Kingdom GSK Investigational Site London, United Kingdom, W1G 6AD 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.81mL 0.36mL 0.18mL |
9.05mL 1.81mL 0.90mL |
18.10mL 3.62mL 1.81mL |
CAS号 | 1315330-11-0 |
分子式 | C29H31F3N6O2 |
分子量 | 552.591 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,2-8°C |
溶解度 |
DMSO: 50 mg/mL(90.48 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 |