1. PROTAC Protein Tyrosine Kinase/RTK
  2. PROTACs TAM Receptor
  3. PROTAC Axl Degrader 2

PROTAC Axl Degrader 2 

目录号: HY-144627 纯度: 98.01%
COA 产品使用指南

PROTAC Axl Degrader 2 是一种有效的选择性 PROTAC Axl 降解剂,IC50 为 1.61 µM。PROTAC Axl Degrader 2 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 2 诱导巨泡式细胞死亡 (mehuosis)。

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PROTAC Axl Degrader 2 Chemical Structure

PROTAC Axl Degrader 2 Chemical Structure

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

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5 mg ¥8000
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 µM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis[1].

IC50 & Target

IC50: 1.61 µM (AXL)[1]

体外研究
(In Vitro)

PROTAC Axl Degrader 2 (compound 20) (72 h) shows anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 2 (0.5, 2 µM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 2 (1, 2 µM) reduces the expression of AXL, can be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 2 (1, 10 µM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 2 (0.5 µM) induces cytoplasmic vacuolation (methuosis) in MDA-MB-231 and 4T1 cells[1].

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

Cell Proliferation Assay[1]

Cell Line: MDA-MB-231, 4T1, GES-1, MCF-10A cells
Concentration:
Incubation Time: 72 h
Result: Showed anti-proliferation activity with IC50s of 6.23 µM, 2.06 µM, for MDA-MB-231, 4T1 cells, respectively.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 2 µM
Incubation Time: 24, 48 h
Result: Decreased AXL abundance in MDA-MB-231 cells.
体内研究
(In Vivo)

PROTAC Axl Degrader 2 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 2 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 7.80%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 2 in 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1].

Cmds Rout Dose (mg/kg) AUC0-t (ng·h/mL) Cmax (ng/mL) Tmax (h) T1/2 (h) CL (L/h/kg) BA (%)
20 i.v. 2 7581.3 279 0.82 1.18 0.72 -
p.o. 20 3592.1 144 2.25 4.43 - 7.80
6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.

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

Animal Model: Female balb/c nude mice (MDA-MB-231 xenografts)[1]
Dosage: 25 mg/kg
Administration: Intraperitoneal injection
Result: Did not induce systemic toxicity.
Animal Model: 6 weeks, 180-220g, male Sprague-Dawley (SD) rats[1]
Dosage:
Administration: 20 mg/kg for o.p.; 2 mg/kg for i.v.
Result: Showed an oral bioavailability of 7.80%.
分子量

713.79

Formula

C38H39N11O4

性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (140.10 mM; 超声助溶; 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 1.4010 mL 7.0049 mL 14.0097 mL
5 mM 0.2802 mL 1.4010 mL 2.8019 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 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
参考文献

PROTAC Axl Degrader 2 相关分类

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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.4010 mL 7.0049 mL 14.0097 mL 35.0243 mL
5 mM 0.2802 mL 1.4010 mL 2.8019 mL 7.0049 mL
10 mM 0.1401 mL 0.7005 mL 1.4010 mL 3.5024 mL
15 mM 0.0934 mL 0.4670 mL 0.9340 mL 2.3350 mL
20 mM 0.0700 mL 0.3502 mL 0.7005 mL 1.7512 mL
25 mM 0.0560 mL 0.2802 mL 0.5604 mL 1.4010 mL
30 mM 0.0467 mL 0.2335 mL 0.4670 mL 1.1675 mL
40 mM 0.0350 mL 0.1751 mL 0.3502 mL 0.8756 mL
50 mM 0.0280 mL 0.1401 mL 0.2802 mL 0.7005 mL
60 mM 0.0233 mL 0.1167 mL 0.2335 mL 0.5837 mL
80 mM 0.0175 mL 0.0876 mL 0.1751 mL 0.4378 mL
100 mM 0.0140 mL 0.0700 mL 0.1401 mL 0.3502 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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产品名称:
PROTAC Axl Degrader 2
目录号:
HY-144627
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