TP-0903 (Synonyms: TP-0903) |
Catalog No.GC14218
One-Click Copy Product Info
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TP-0903 (TP-0903) est un inhibiteur puissant et sélectif de la tyrosine kinase du récepteur Axl avec une valeur IC50 de 27 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1341200-45-0
Sample solution is provided at 25 µL, 10mM.
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Description:
IC50: 0.027 μM against AXL
AXL and other TAM family members are known to be involved in maintaining the mesenchymal phenotype in cancer cells. Mesenchymal cells have increased invasion and migratory properties, enhanced cell survival in stressed environments, as well as increased resistance to targeted therapies. TP-0903 is a potent anti-cancer agent targeting the AXL receptor tyrosine kinase.
In vitro: On the basis of the potency of TP-0903 in biochemical assays, its activity in cell-based studies was evaluated. TP-0903 showed extremely potent activity in cell viability assays against the pancreatic cancer cell line PSN-1. More importantly, TP-0903 was evaluated for its ability to block GAS6-mediated activation of AXL in pancreatic cancer cells. PSN-1 cells were serum-starved and then stimulated with GAS6 in the presence of various concentrations of TP-0903 [1].
In vivo: TP-0903 restores sensitivity to erlotinib in cell-based and preclinical animal models of cancer by reversing the mesenchymal phenotype driving resistance [2].
Clinical trial: Up to now, TP-0903 is still in the preclinical development stage.
Reference:
[1] Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912.
[2] ToleroPharmaceuticals, Inc–TP-0903. http://www.toleropharmaceuticals.com/TP-0903.html.
Cell experiment: | 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]. |
References: [1]. Mollard A, et al. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912. | |
| Cas No. | 1341200-45-0 | SDF | |
| Synonymes | TP-0903 | ||
| Chemical Name | (E)-2-((5-chloro-2-((4-((4-methylpiperazin-1-yl)methyl)phenyl)amino)pyrimidin-4(3H)-ylidene)amino)-N,N-dimethylbenzenesulfonamide | ||
| Canonical SMILES | CN(S(C1=CC=CC=C1/N=C(N2)\C(Cl)=CN=C2NC3=CC=C(CN4CCN(CC4)C)C=C3)(=O)=O)C | ||
| Formula | C24H30ClN7O2S | M.Wt | 516.06 |
| Solubility | ≥ 25.8mg/mL in DMSO with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9378 mL | 9.6888 mL | 19.3776 mL |
| 5 mM | 387.6 μL | 1.9378 mL | 3.8755 mL |
| 10 mM | 193.8 μL | 968.9 μL | 1.9378 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)