2. Protein Tyrosine Kinase/RTK Apoptosis
  3. TAM Receptor Apoptosis
  4. Dubermatinib

Dubermatinib  (Synonyms: TP-0903)

Cat. No.: HY-12963 Purity: 99.84%
SDS COA Handling Instructions

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Dubermatinib (TP-0903) is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.

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

Dubermatinib Chemical Structure

Dubermatinib Chemical Structure

CAS No. : 1341200-45-0

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1 mg USD 36 In-stock
5 mg USD 77 In-stock
10 mg USD 110 In-stock
50 mg USD 319 In-stock
100 mg USD 495 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Dubermatinib Related Antibodies

Top Publications Citing Use of Products

View All TAM Receptor Isoform Specific Products:

View All Isoforms
Axl Mer Tyro3

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Dubermatinib (TP-0903) is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.

IC50 & Target

Axl

 

Cellular Effect
Cell Line Type Value Description References
PSN1 IC50
0.06 μM
Compound: 13
Cytotoxicity against human PSN1 cells after 96 hrs by ATP-lite luminescence assay
Cytotoxicity against human PSN1 cells after 96 hrs by ATP-lite luminescence assay
[PMID: 22247788]
PSN1 EC50
222 nM
Compound: 13
Inhibition of AXL in human PSN1 cells assessed as decrease in GAS6-induced phospho-AXL level after 2 hrs by EILSA
Inhibition of AXL in human PSN1 cells assessed as decrease in GAS6-induced phospho-AXL level after 2 hrs by EILSA
[PMID: 22247788]
PSN1 EC50
305 nM
Compound: 13
Inhibition of AXL-mediated AKT Ser473 phosphorylation in human PSN1 cells assessed as decrease in GAS6-induced phospho-AKT level after 2 hrs by ELISA
Inhibition of AXL-mediated AKT Ser473 phosphorylation in human PSN1 cells assessed as decrease in GAS6-induced phospho-AKT level after 2 hrs by ELISA
[PMID: 22247788]
In Vitro

Dubermatinib (TP-0903) displays a potent activity against AXL with an IC50 of 0.027 μM. Dubermatinib (TP-0903) shows extremely potent activity in cell viability assays with an IC50 of 6 nM against the pancreatic cancer cell line PSN-1. Dubermatinib (TP-0903) is evaluated for its ability to block GAS6-mediated activation of AXL in pancreatic cancer cells. PSN-1 cells are serum-starved and then stimulated with GAS6 in the presence of various concentrations of TP-0903[1].

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

Dubermatinib Related Antibodies
Clinical Trial
Molecular Weight

516.06

Formula

C24H30ClN7O2S
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=S(C1=CC=CC=C1NC2=NC(NC3=CC=C(CN4CCN(C)CC4)C=C3)=NC=C2Cl)(N(C)C)=O
Shipping

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

DMSO : 2 mg/mL (3.88 mM; ultrasonic and warming and heat to 60°C; 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 1.9378 mL 9.6888 mL 19.3776 mL
5 mM --- --- ---
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  0.5% CMC-Na/saline water

    Solubility: 10 mg/mL (19.38 mM); Suspended solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.84%

SDS (393 KB)

COA (247 KB) HNMR (267 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

For cell proliferation assays, 45 μL containing 1000 cells per well are seeded into solid white 384-well plates in appropriate media. The following day, Dubermatinib (TP-0903) is diluted in serum free growth media to 10x desired concentrations and 5 μL is added to each well. Combined compound and cells are incubated for 96 hours. Following incubation, 40 μL of ATP-Lite solution is added to each well, incubated for an additional 10 minutes at room temperature and luminescence is measured on an microplate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9378 mL 9.6888 mL 19.3776 mL 48.4440 mL
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Dubermatinib 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:

Dubermatinib1341200-45-0TP-0903TP0903TP 0903TAM ReceptorApoptosisTyro3AxlMerInhibitorinhibitorinhibit

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