AZ304 is an inhibitor of BRAF and can target many kinases. The IC50s for wild type BRAF, V600E mutant BRAF and wild type CRAF are 79 nM, 38 nM and 68 nM, respectively. It can also inhibit p38 (IC50 = 6 nM) and CSF1R (IC50 = 35 nM).
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产品名称 | p38 MAPK ↓ ↑ | p38α ↓ ↑ | p38β ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BMS-582949 |
+++
p38 MAPK, IC50: 13 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SB 203580 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
Pexmetinib | ✔ | Tie-2 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Skepinone-L |
++++
p38α, IC50: 5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Doramapimod |
++++
p38α, IC50: 38 nM p38α, Kd: 0.1 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
VX-702 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
Ralimetinib dimesylate |
++++
p38α, IC50: 7 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SB 202190 |
++
p38α, IC50: 50 nM |
++
p38β, IC50: 100 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Losmapimod |
++++
p38α, pKi: 8.1 |
+++
p38β, pKi: 7.6 |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Neflamapimod |
+++
p38α, IC50: 10 nM |
+
p38β, IC50: 220 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
PH-797804 |
++
p38α, IC50: 26 nM |
+
p38β, IC50: 102 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
TAK-715 |
++++
p38α, IC50: 7.1 nM |
+
p38β, IC50: 0.20 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
SB 239063 |
++
p38α, IC50: 44 nM |
++
p38β, IC50: 44 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Pamapimod |
+++
p38α, IC50: 0.014 μM |
+
p38β, IC50: 0.48 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
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。 |
产品名称 | A-raf ↓ ↑ | B-Raf ↓ ↑ | C-Raf/Raf-1 ↓ ↑ | Raf ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Encorafenib | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
GDC-0879 |
++++
B-Raf, IC50: 0.13 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
SB-590885 |
++++
B-Raf, Ki: 0.16 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
RAF265 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
Dabrafenib |
++++
B-Raf, IC50: 5.2 nM B-Raf (V600E), IC50: 0.7 nM |
+++
C-Raf, IC50: 6.3 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
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 | {[allProObj[0].p_purity_real_show]} | ||||||||||||||
ZM 336372 |
+
C-Raf, IC50: 70 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
NVP-BHG 712 |
+
C-Raf, IC50: 0.395 μM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
CCT196969 |
+
BRAF, IC50: 0.1 μM |
++
CRAF, IC50: 0.01 μM |
Src | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
Vemurafenib |
++
B-Raf, IC50: 100 nM B-Raf (V600E), IC50: 31 nM |
+
C-Raf, IC50: 48 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
PLX4720 |
++
B-Raf, IC50: 160 nM B-Raf (V600E), IC50: 13 nM |
+++
C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM |
BRK | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
GW 5074 |
+++
C-Raf, IC50: 9 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Avutometinib |
+++
BRAF V600E, IC50: 8.2 nM BRAF, IC50: 19 nM |
+
CRAF, IC50: 56 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
LY3009120 |
++++
BRAF WT, IC50: 15 nM BRAF(V600E), IC50: 5.8 nM |
++++
C-Raf, IC50: 4.3 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Agerafenib |
++
B-Raf (V600E), Kd: 14 nM B-Raf, Kd: 36 nM |
+
C-Raf, Kd: 39 nM |
RET | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
TAK-632 |
+++
B-Raf, IC50: 8.3 nM |
++++
C-Raf, IC50: 1.4 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
AZ 628 |
+
B-Raf, IC50: 105 nM B-Raf (V600E), IC50: 34 nM |
++
C-Raf-1, IC50: 29 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
PLX7904 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Sorafenib |
++
B-Raf (V599E), IC50: 38 nM B-Raf, IC50: 22 nM |
++++
Raf-1, IC50: 6 nM |
++++
Raf-1, IC50: 6 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||
Tovorafenib | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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 | AZ304 is a dual BRAF inhibitor, with IC50 values of 38, 79, 68, 6 and 35nM for BRAFV600E, BRAF, CRAF, p38 and CSF1R, respectively, exerting potent inhibitory effects on both wild type and V600E mutant forms of the serine/threonine-protein kinase BRAF. AZ304 at concentration<1μM effectively inhibited a panel of human cancer cell lines with different BRAF and RAS genetic statuses, by suppressing ERK phosphorylation. The anti-proliferative activity of AZ304 cannot be retained by EGF in CRC cell lines with different BRAF mutation status. Oral gavage with 10mg/kg AZ304, twice daily, for 10 days, exhibited anti-tumour activity in RKO and Caco-2 xenograft model. And combination of Cetuximab with AZ304 could enhance this anti-tumour activity[2]. |
Dose | Nude Mice: 10 mg/kg[1] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.21mL 0.44mL 0.22mL |
11.07mL 2.21mL 1.11mL |
22.15mL 4.43mL 2.21mL |
CAS号 | 942507-42-8 |
分子式 | C27H25N5O2 |
分子量 | 451.52 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 120 mg/mL(265.77 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 |