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

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.

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PROTAC Axl Degrader 2 Chemical Structure

PROTAC Axl Degrader 2 Chemical Structure

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Based on 1 publication(s) in Google Scholar

PROTAC Axl Degrader 2 Related Antibodies

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Description

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]
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].

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

PROTAC Axl Degrader 2 Related Antibodies

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.
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.

MedChemExpress (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%.
Molecular Weight

713.79

Formula

C38H39N11O4
Appearance

Solid

Color

White to light yellow

SMILES

NC1=NC(NC2=CC=C(C=C2)CNC(CCCCCNC3=CC=CC4=C3CN(C4=O)C5CCC(NC5=O)=O)=O)=NN1C6=CC=C(N=N6)C7=CC=CC=C7
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

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

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (140.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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
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PROTAC Axl Degrader 2 Related Classifications

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.

Keywords:

PROTAC Axl Degrader 2PROTAC Axl Degrader2PROTAC Axl Degrader-2PROTACsTAM ReceptorTyro3AxlMerSelectiveanti-tumorMDA-MB-231 xenograftsSprague-Dawley (SD) ratsepoxymycinmigrationMDA-MB-231 cellsInhibitorinhibitorinhibit

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