LXS196 is a potent and orally active protein kinase C (PKC) inhibitor used for the treatment of uveal melanoma.
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 纯度 | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
LDN193189 |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99%+ | ||||||||||||||
LDN-212854 |
++++
ALK1, IC50: 2.4 nM |
++++
ALK2, IC50: 1.3 nM |
+
ALK3, IC50: 85.8 nM |
+
ALK4, IC50: 2133 nM |
+
ALK5, IC50: 9276 nM |
99%+ | |||||||||||||
ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
98% | ||||||||||||||||
K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
99%+ | ||||||||||||||
LDN-193189 dihydrochloride |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99% | ||||||||||||||
LDN-214117 |
++
ALK2, IC50: 24 nM |
98% | |||||||||||||||||
DMH-1 |
+
ALK2, IC50: 107.9 nM |
99%+ | |||||||||||||||||
SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
99%+ | ||||||||||||||||
Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
99%+ | ||||||||||||||||
Alantolactone | ✔ | 98% | |||||||||||||||||
SIS3 | ✔ | 97% | |||||||||||||||||
Pirfenidone | ✔ | 98% | |||||||||||||||||
Hesperetin | ✔ | 97% | |||||||||||||||||
RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
98% | |||||||||||||||||
GW788388 |
+++
ALK5, IC50: 18 nM |
98% | |||||||||||||||||
LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
98% | ||||||||||||||||
SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
98% | |||||||||||||||||
SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
99%+ | |||||||||||||||||
LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
99%+ | ||||||||||||||||
Galunisertib |
++
TβRI, IC50: 56 nM |
98% | |||||||||||||||||
SB 431542 |
+
ALK5, IC50: 94 nM |
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。 |
产品名称 | PKC ↓ ↑ | PKCα ↓ ↑ | PKCβ ↓ ↑ | PKCγ ↓ ↑ | PKCδ ↓ ↑ | PKCε ↓ ↑ | PKCζ ↓ ↑ | PKCη ↓ ↑ | PKCθ ↓ ↑ | 其他靶点 | 纯度 | ||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Daphnetin |
+
PKC, IC50: 25.01 μM |
EGFR,PKA | 95% | ||||||||||||||||
Dequalinium Chloride | 99%+ | ||||||||||||||||||
Quercetin | ✔ | Src,Sirtuin | 97% | ||||||||||||||||
Myricetrin | ✔ | 96% | |||||||||||||||||
Go 6983 |
+++
PKCα, IC50: 7 nM |
+++
PKCβ, IC50: 7 nM |
+++
PKCγ, IC50: 6 nM |
+++
PKCδ, IC50: 10 nM |
++
PKCζ, IC50: 60 nM |
99%+ | |||||||||||||
Go6976 |
+++
PKC, IC50: 7.9 nM |
++++
PKCα, IC50: 2.3 nM |
+++
PKCβ1, IC50: 6.2 nM |
FLT3 | 99%+ | ||||||||||||||
Bisindolylmaleimide I |
+++
PKCα, IC50: 20 nM |
+++
PKCβ2, IC50: 16 nM PKCβ1, IC50: 17 nM |
+++
PKCγ, IC50: 20 nM |
99%+ | |||||||||||||||
Lawsone methyl ether | ✔ | 99% | |||||||||||||||||
Sotrastaurin |
++++
PKCα, Ki: 0.95 nM |
++++
PKCβ1, Ki: 0.64 nM |
++++
PKCδ, Ki: 2.1 nM |
++++
PKCε, Ki: 3.2 nM |
++++
PKCη, Ki: 1.8 nM |
++++
PKCθ, Ki: 0.22 nM |
99%+ | ||||||||||||
Enzastaurin |
++
PKCα, IC50: 39 nM |
+++
PKCβ, IC50: 6 nM |
+
PKCγ, IC50: 83 nM |
+
PKCε, IC50: 110 nM |
98% | ||||||||||||||
Midostaurin |
++
PKCα, IC50: 22 nM |
++
PKCβ2, IC50: 31 nM PKCβ1, IC50: 30 nM |
++
PKCγ, IC50: 24 nM |
+
PKCδ, IC50: 330 nM |
+
PKCε, IC50: 1.25 μM |
+
PKCη, IC50: 160 nM |
99% | ||||||||||||
Ro 31-8220 mesylate |
++++
PKCα, IC50: 5 nM |
+++
PKCβ2, IC50: 14 nM PKCβ1, IC50: 24 nM |
++
PKCγ, IC50: 27 nM |
++
PKCε, IC50: 24 nM |
99%+ | ||||||||||||||
Staurosporine |
++++
PKCα, IC50: 2 nM |
++++
PKCγ, IC50: 5 nM |
+++
PKCδ, IC50: 20 nM |
++
PKCε, IC50: 73 nM |
++++
PKCη, IC50: 4 nM |
99%+ | |||||||||||||
Ruboxistaurin HCl |
+
PKCα, IC50: 0.36 μM |
++++
PKCβ2, IC50: 5.9 nM PKCβ1, IC50: 4.7 nM |
+
PKCγ, IC50: 0.3 μM |
+
PKCδ, IC50: 0.25 μM |
++
PKCη, IC50: 0.052 μM |
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 | Darovasertib, also known as LXS196, is an effective, selective, orally active PKC inhibitor, with IC50 values of 1.9 nM for PKCα, 0.4 nM for PKCθ, and 3.1 μM for GSK3β. Darovasertib holds potential for research in uveal melanoma[1][2]. Upon oral administration, Darovasertib binds to and inhibits PKC, thereby preventing the activation of PKC-mediated signaling pathways. This may result in cell cycle arrest and the induction of apoptosis in sensitive tumor cells[1]. |
Animal study | Administered orally at doses of 15, 30, 75, and 150 mg/kg, Darovasertib demonstrates dose-dependent improved efficacy (regression) in the 92.1 GNAQ uveal melanoma xenograft mouse model[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.12mL 0.42mL 0.21mL |
10.58mL 2.12mL 1.06mL |
21.17mL 4.23mL 2.12mL |
CAS号 | 1874276-76-2 |
分子式 | C22H23F3N8O |
分子量 | 472.466 |
别名 | Lxs196;IDE196 |
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: 25 mg/mL(52.91 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 |