1. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK
  2. Raf Src Ribosomal S6 Kinase (RSK) RET
  3. AD80

AD80 是多种激酶的抑制剂,抑制 RETRAFSRCS6K 活性,但对 mTOR 的活性明显减弱。

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AD80 Chemical Structure

AD80 Chemical Structure

CAS No. : 1384071-99-1

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1200
In-stock
5 mg ¥1150
In-stock
10 mg ¥1850
In-stock
25 mg ¥3700
In-stock
50 mg ¥5165
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

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查看 Ribosomal S6 Kinase (RSK) 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

AD80, a multikinase inhibitor, inhibits RET, RAF,SRCand S6K, with greatly reduced mTOR activity.

IC50 & Target[1]

p70S6K

 

RAF

 

RET

 

SRC

 

体外研究
(In Vitro)

AD80 is a polypharmacological agent with an optimal balance of activity against Ret, Raf, Src, Tor and S6K that show high efficacy with very low toxicity. AD80 and AD81 inhibits RET, RAF, SRC and S6K, with greatly reduced mTOR activity relative to AD57 and AD58.AD80 is optimal for Ras–Erk pathway inhibition. AD80 inhibits proliferation of MZ-CRC-1 and TT thyroid cancer cells in culture, probably through the induction of apoptosis. Immunoblot analysis demonstrates potent downregulation of phosphorylated Ret and several downstream biomarkers within these cells[1]. AD80 coordinately inhibits S6K1 together with the TAM family tyrosine kinase AXL.AD80 avoides S6K1 phosphorylation and mTOR co-association, resulting in durable suppression of S6K1-induced signaling and protein synthesis[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Oral administration of either AD80 or AD81 results in a notable 70-90% of animals developing to adulthood in Drosophila ptc>dRetMEN2Bmodel, a considerable improvement over the efficacy observed with AD57. AD80 also promotes enhanced tumour growth inhibition and reduces body-weight modulation relative to vandetanib in a mouse xenograft model[1]. AD80 rescues 50% of mice transplanted with PTEN-deficient leukemia cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

473.43

Formula

C22H19F4N7O

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (105.61 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1122 mL 10.5612 mL 21.1224 mL
5 mM 0.4224 mL 2.1122 mL 4.2245 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.88%

参考文献
Cell Assay
[1]

MZ-CRC-1 (MEN2B) and TT (MEN2A) cells are treated with AD80 (0.2 nM to 20 μM) for 7 days and cell viability is quantitated by MTT assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Mice:
Mice showing established growing tumors are separated into vehicle or drug treatment groups. A similar range of tumor sizes is selected for each experiment (vehicle vs AD57; vehicle vs AD80 vs Vandetanib). Vehicle, AD57 (20 mg/kg), AD80 (30 mg/kg), or Vandetanib (50mg/kg) are administered by oral gavage (PO; per os or by mouth) once daily, five times a week. Tumor and body weight measurements are performed 3 times a week[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1122 mL 10.5612 mL 21.1224 mL 52.8061 mL
5 mM 0.4224 mL 2.1122 mL 4.2245 mL 10.5612 mL
10 mM 0.2112 mL 1.0561 mL 2.1122 mL 5.2806 mL
15 mM 0.1408 mL 0.7041 mL 1.4082 mL 3.5204 mL
20 mM 0.1056 mL 0.5281 mL 1.0561 mL 2.6403 mL
25 mM 0.0845 mL 0.4224 mL 0.8449 mL 2.1122 mL
30 mM 0.0704 mL 0.3520 mL 0.7041 mL 1.7602 mL
40 mM 0.0528 mL 0.2640 mL 0.5281 mL 1.3202 mL
50 mM 0.0422 mL 0.2112 mL 0.4224 mL 1.0561 mL
60 mM 0.0352 mL 0.1760 mL 0.3520 mL 0.8801 mL
80 mM 0.0264 mL 0.1320 mL 0.2640 mL 0.6601 mL
100 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5281 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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