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

PROTAC Axl Degrader 1 是一种有效的选择性 PROTAC Axl 降解剂,IC50 为 0.92 μM。PROTAC Axl Degrader 1 显示出体外抗增殖活性、抗迁移活性。PROTAC Axl Degrader 1 诱导巨泡式细胞死亡。

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PROTAC Axl Degrader 1 Chemical Structure

PROTAC Axl Degrader 1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis[1].

IC50 & Target

Axl

 

体外研究
(In Vitro)

PROTAC Axl Degrader 1 (compound 22) (72 h) shows anti-proliferation activity with IC50s of 10.34 μM, 5.53 μM, for MDA-MB-231, 4T1 cells, respectively[1].
PROTAC Axl Degrader 1 (0.5, 2 μM; 24, 48 h) decreases the abundance of AXL in MDA-MB-231 cells[1].
PROTAC Axl Degrader 1 (1, 2 μM) reduces the expression of AXL, could be restored in the presence of EPO (epoxymycin)[1].
PROTAC Axl Degrader 1 (1, 10 μM; 48 h) significantly inhibits the migration in MDA-MB-231 and 4T1 cells[1].
PROTAC Axl Degrader 1 (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 10.34 µM, 5.53 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 1 (25 mg/kg, i.p.) dose not induce systemic toxicity[1].
PROTAC Axl Degrader 1 (20 mg/kg for o.p.; 2 mg/kg for i.v.) shows an oral bioavailability of 4.93%[1].
Pharmacokinetic Parameters of PROTAC Axl Degrader 1 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 (%)
22 i.v. 2 2933.4 166 0.54 0.72 0.68 -
p.o. 20 864.7 92 1.89 2.37 - 4.93
6 weeks, 180-220g, male Sprague-Dawley (SD) rats; 20 mg/kg for o.p.; 2 mg/kg for i.v.[1].

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

分子量

741.84

Formula

C40H43N11O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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 1
目录号:
HY-144624
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