2. Protein Tyrosine Kinase/RTK Neuronal Signaling
  3. TAM Receptor c-Met/HGFR Trk Receptor
  4. DS-1205b free base

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo.

For research use only. We do not sell to patients.

DS-1205b free base Chemical Structure

DS-1205b free base Chemical Structure

CAS No. : 1855860-24-0

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 534 In-stock
Solution
10 mM * 1 mL in DMSO USD 534 In-stock
Solid
5 mg USD 330 In-stock
10 mg USD 495 In-stock
25 mg USD 891 In-stock
50 mg USD 1247 In-stock
100 mg USD 1745 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

DS-1205b free base Related Antibodies

Top Publications Citing Use of Products

View All TAM Receptor Isoform Specific Products:

View All Isoforms
Axl Mer Tyro3

View All Trk Receptor Isoform Specific Products:

View All Isoforms
TrkA TrkB TrkC Trk

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo[1].

IC50 & Target[1]

Axl

 

Mer

 

AXL

1.3 nM (IC50)

MER

63 nM (IC50)

TrkA

407 nM (IC50)

Met

104 nM (IC50)

In Vitro

DS-1205b (0.3-33 μM; 2-24 h) inhibits hGAS6-induced migration in NIH3T3-AXL cells (EC50=2.7 nM)[1].
DS-1205b (1-10000 μM; 2-24 h) significantly inhibits the phosphorylation of AXL in NIH3T3-AXL cells. DS-1205b decreases NIH3T3 cell proliferation but not obviously inhibits growth (GI50>10,000 nM)[1].

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

DS-1205b free base Related Antibodies

Western Blot Analysis[1]

Cell Line: NIH3T3-AXL cells
Concentration: 1, 10, 100, 1000, 10000 μM
Incubation Time: 2, 24 hours
Result: Completely inhibited the phosphorylation of AXL at concentrations above 10 nM.
Slightly inhibited the phosphorylation of AKT serine/threonine kinase in a dose-dependent manner.
In Vivo

DS-1205b (3.1-50 mg/kg; p.o. bid for 5 d) exhibits pAXL inhibition mediated antitumor effects in mice[1].

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

Animal Model: Female NOD/Shi-scid IL-2Rγ KO Jic mice were implanted with NIH3T3-AXL tumor blocks[1]
Dosage: 3.1, 6.3, 13, 25, 50 mg/kg
Administration: P.o. twice daily for 5 days
Result: Inhibited tumor growth by 39-94%.
Reduced the phosphorylation of both AXL and AKT in tumors.
Molecular Weight

735.80

Formula

C41H42FN5O7
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=CN(CC2CCOCC2)C=C(C3=NC=C(C)C=C3)C1=O)NC4=CC=C(C5=CC(C6=CC=C(OC[C@@H]7OCCOC7)C(OC)=C6)=CN=C5N)C(F)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (67.95 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 1.3591 mL 6.7953 mL 13.5907 mL
5 mM 0.2718 mL 1.3591 mL 2.7181 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.92%

COA (247 KB) HNMR (220 KB) LCMS (112 KB)

Handling Instructions (2659 KB)
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. 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 1.3591 mL 6.7953 mL 13.5906 mL 33.9766 mL
5 mM 0.2718 mL 1.3591 mL 2.7181 mL 6.7953 mL
10 mM 0.1359 mL 0.6795 mL 1.3591 mL 3.3977 mL
15 mM 0.0906 mL 0.4530 mL 0.9060 mL 2.2651 mL
20 mM 0.0680 mL 0.3398 mL 0.6795 mL 1.6988 mL
25 mM 0.0544 mL 0.2718 mL 0.5436 mL 1.3591 mL
30 mM 0.0453 mL 0.2265 mL 0.4530 mL 1.1326 mL
40 mM 0.0340 mL 0.1699 mL 0.3398 mL 0.8494 mL
50 mM 0.0272 mL 0.1359 mL 0.2718 mL 0.6795 mL
60 mM 0.0227 mL 0.1133 mL 0.2265 mL 0.5663 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

DS-1205b free base 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:

DS-1205b1855860-24-0TAM Receptorc-Met/HGFRTrk ReceptorTyro3AxlMerTropomyosin related kinase receptorAXLkinaseMERMETTRKAmigrationtumorNIH3T3Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
DS-1205b free base
Cat. No.:
HY-114357A
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.