
TPX-0046 CAS No.:2359650-19-2
TPX-0046 (TPX0046) is a potent, selective next-generation RET/SRC inhibitor, demonstrates low nanomolar potency against WT and 18 RET mutations/fusions, as well as SRC, and is VEGFR2/KDR-sparing.
Description
for this product.
Introduction:
TPX-0046 CAS No.:2359650-19-2 is a research chemical that is widely used for various laboratory and research purposes. Its high purity and excellent quality make it an ideal choice for many scientists and researchers who are looking for a reliable and efficient chemical for their experiments. TPX-0046 is also known by its chemical name, (2R,3R,6R)-2-(2,4-difluorophenyl)-N,6-dimethyl-5-oxo-2,3,6,9-tetrahydro-1H-pyridine-3-carboxamide.
Properties:
TPX-0046 is a white or off-white crystalline powder that is soluble in dimethyl sulfoxide (DMSO) and methanol. It has a molecular weight of 337.4 g/mol and a purity level of 99% or higher.
Usage:
TPX-0046 is mainly used in the research and development of pharmaceuticals, especially in the discovery of new drugs. It is also used in academic and research institutions for various scientific research and studies, including proteomics research, drug discovery, and screening of new compounds.
Benefits:
Some of the main benefits of using TPX-0046 in research and development include its high purity, excellent quality, and low toxicity. It is also highly stable and resistant to degradation, which enables it to be stored for long periods without losing its potency or effectiveness. Additionally, TPX-0046 has been shown to have a wide range of applications in the pharmaceutical industry, making it a highly versatile and valuable research tool.
Safety:
TPX-0046 is classified as a research chemical and should only be used by trained professionals in a laboratory setting. While it has a low toxicity level, appropriate safety precautions should still be taken when handling and using it, including wearing protective clothing, using proper ventilation, and following standard laboratory procedures.
Conclusion:
TPX-0046 CAS No.:2359650-19-2 is an excellent research chemical that is highly valued by scientists and researchers in a wide range of fields, including pharmaceuticals, proteomics research, and drug discovery. Its high purity, excellent quality, and low toxicity make it an ideal choice for those who require a reliable and efficient chemical for their experiments. If you are looking for a high-quality and versatile research chemical that can help you achieve your research goals, then TPX-0046 is a great choice.

TPX-0046 (TPX0046)
Catalog No.: URK-V871 Only Used For Lab.
TPX-0046 (TPX0046) is a potent, selective next-generation RET/SRC inhibitor, demonstrates low nanomolar potency against WT and 18 RET mutations/fusions, as well as SRC, and is VEGFR2/KDR-sparing.
Biological Activity
TPX-0046 (TPX0046) is a potent, selective next-generation RET/SRC inhibitor, demonstrates low nanomolar potency against WT and 18 RET mutations/fusions, as well as SRC, and is VEGFR2/KDR-sparing.
TPX-0046 inhibited RET phosphorylation (IC50 < 10 nM) in tumor cell lines (LC2/ad, CCDC6-RET; TT, RET C634W) and Ba/F3 engineered RET models (WT, G810R).
TPX-0046 inhibited KIF5B-RET Ba/F3, LC2/ad, and TT cells with IC50 values of 1 nM in cell proliferation assays.
TPX-0046 potently inhibited Ba/F3 RET engineered cells with SFMs (e.g. G810C/R/S) with mean proliferation IC50 of 1-17 nM.
TPX-0046 demonstrated marked in vivo anti-tumor efficacy in RET-driven cell-derived and patient-derived xenograft tumor models, a single dose of 5 mg/kg TPX-0046 inhibited >80% of RET phosphorylation.
TPX-0046 is a unique next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFM-mediated resistance.
Physicochemical Properties
|
M.Wt |
424.436 |
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Formula |
C21H21FN6O3 |
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CAS No. |
2359650-19-2 |
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Storage |
Solide Powder -20 °C 3years; 4°C 2years |
In Solvent -80°C 6 Months -20°C 1 Months |
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Solubility |
10 mM in DMSO |
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Chemical Name |
(13E,14E,15aS,18aR,5R)-35-fluoro-5-methyl-15,15a,16,17,18,18a-hexahydro-4-oxa-7-aza-1(5,3)-cyclopenta[b]pyrazolo[1',5':1,2]pyrimido[4,5-e][1,4]oxazina-3(3,2)-pyridinacyclooctaphan-8-one |
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References
1. A.Drilon, et al. Annals of Oncology Volume 30, Supplement 5, October 2019, Pages v190-v191
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