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TAK1/MAP4K2 inhibitor 1 {[allProObj[0].p_purity_real_show]}

货号:A756511

B-Raf inhibitor, a pyrazine and pyrrolo[2,3-b]pyridine derivative, is useful in the treatment of cancer and proliferative diseases.

TAK1/MAP4K2 inhibitor 1 化学结构 CAS号:1315330-11-0
TAK1/MAP4K2 inhibitor 1 化学结构
CAS号:1315330-11-0
TAK1/MAP4K2 inhibitor 1 3D分子结构
CAS号:1315330-11-0
TAK1/MAP4K2 inhibitor 1 化学结构 CAS号:1315330-11-0
TAK1/MAP4K2 inhibitor 1 3D分子结构 CAS号:1315330-11-0
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TAK1/MAP4K2 inhibitor 1 纯度/质量文件 产品仅供科研

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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。

TAK1/MAP4K2 inhibitor 1 生物活性

描述 B-Raf inhibitor, a pyrazine and pyrrolo[2,3-b]pyridine derivative, is useful in the treatment of cancer and proliferative diseases.

TAK1/MAP4K2 inhibitor 1 临床研究

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 <<

TAK1/MAP4K2 inhibitor 1 参考文献

[1]Herr R, Kohler M, et al. B-Raf inhibitors induce epithelial differentiation in BRAF-mutant colorectal cancer cells. Cancer Res. 2015 Jan 1;75(1):216-29.

[2]Arora R, Di Michele M, et al. Structural investigation of B-Raf paradox breaker and inducer inhibitors. J Med Chem. 2015 Feb 26;58(4):1818-31.

TAK1/MAP4K2 inhibitor 1 实验方案

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

TAK1/MAP4K2 inhibitor 1 技术信息

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
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