
Pemigatinib CAS No.:1513857-77-6
Chemical Structure : Pemigatinib
CAS No.: 1513857-77-6
Description
Welcome to our product introduction for Pemigatinib, CAS No.: 1513857-77-6. As a leading manufacturer based in China, we are proud to offer this innovative and high-quality product to merchants across the world. In this introduction, we will provide you with key information about Pemigatinib, including its benefits, usage, and unique features.
Overview of Pemigatinib
Pemigatinib is a small molecule inhibitor that targets FGFR (Fibroblast Growth Factor Receptor) proteins, which are implicated in the growth and survival of various cancers. Specifically, Pemigatinib targets the FGFR2 and FGFR3 proteins, which are commonly mutated in cholangiocarcinoma, a type of bile duct cancer, as well as other solid tumors.
Pemigatinib was initially developed by Incyte Corporation, a pharmaceutical company based in the United States, and has been approved by the U.S. Food and Drug Administration (FDA) for the treatment of locally advanced or metastatic cholangiocarcinoma with FGFR2 fusion or rearrangement, following progression on chemotherapy. It has also been granted Orphan Drug Designation by the FDA for the treatment of cholangiocarcinoma and intrahepatic cholangiocarcinoma.
Benefits of Pemigatinib
The primary benefit of Pemigatinib is its ability to slow down or halt the progression of cholangiocarcinoma, a particularly difficult-to-treat cancer, in patients with FGFR2 fusion or rearrangement. In a phase 2 clinical trial conducted by Incyte, Pemigatinib was shown to achieve a 36% overall response rate, as well as a median progression-free survival of 6.9 months among patients with advanced cholangiocarcinoma.
In addition to its anti-cancer properties, Pemigatinib may also have potential applications in treating other FGFR-related diseases, such as bladder cancer and multiple myeloma. Several clinical trials are currently underway to investigate these possibilities.
Usage and Dosage of Pemigatinib
Pemigatinib is an oral medication that comes in the form of tablets, with strengths of 4.5 mg, 9 mg, or 13.5 mg. The recommended daily dose of Pemigatinib for the treatment of cholangiocarcinoma is 13.5 mg, taken once daily, with or without food.
It is important to note that Pemigatinib can cause several side effects, such as fatigue, nausea, vomiting, diarrhea, and elevated liver enzymes. Patients taking Pemigatinib should be monitored closely for signs of these side effects.
Unique Features of Pemigatinib
Pemigatinib stands out from other cancer treatments due to its high selectivity for FGFR2 and FGFR3 proteins, which are not commonly targeted by other cancer therapies. This specificity allows Pemigatinib to precisely target and inhibit cancer cells, while avoiding damage to healthy cells.
Another unique feature of Pemigatinib is its availability as an oral medication, which offers convenience to patients who may have difficulty with intravenous treatments. Additionally, unlike some traditional chemotherapy agents, Pemigatinib has a lower risk of causing hair loss or other visible side effects.
Conclusion
In summary, Pemigatinib is a highly selective and effective small molecule inhibitor that has been approved for the treatment of advanced cholangiocarcinoma with FGFR2 fusion or rearrangement. As a manufacturer based in China, we are proud to offer this innovative and life-changing product to merchants around the world. Whether you are a medical professional seeking new treatments for your patients, or a distributor looking to expand your product line, we believe that Pemigatinib can provide real value and benefits to your business and clients.
Chemical Structure : Pemigatinib
CAS No.: 1513857-77-6

Pemigatinib (INCB054828;INCB 054828)
Catalog No.: URK-V620 Only Used For Lab.
Pemigatinib (INCB054828, INCB 054828) is a potent, selective, orally bioavailable inhibitor of FGFR1/2/3, potently inhibits the kinase activity of recombinant FGFR1, FGFR2 and FGFR3 enzymes and is highly selective against a panel of kinases including VEGFR2.
Biological Activity
Pemigatinib (INCB054828, INCB 054828) is a potent, selective, orally bioavailable inhibitor of FGFR1/2/3, potently inhibits the kinase activity of recombinant FGFR1, FGFR2 and FGFR3 enzymes and is highly selective against a panel of kinases including VEGFR2; inhibits the autophosphorylation of FGFR proteins with low nanomolar IC50 values and blocks signal transduction by FGFR to downstream markers of pathway activation. Cancer cell lines that have genetic alterations in FGFR1, FGFR2 and FGFR3 were uniquely displays sensitivity to cancer cell growth that have genetic alterations in FGFR1, FGFR2 and FGFR3 with IC50 in the range of 3-50 nM, with little to no effect on cancer cell lines or normal cells without FGFR dependence (IC50>1.5 uM); inhibits the growth of tumors that are dependent upon FGFR1, FGFR2 and FGFR3 activity in vivo, which is dose-dependent and correlated with pharmacodynamic inhibition of FGFR.
Physicochemical Properties
|
M.Wt |
487.5 |
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Formula |
C24H27F2N5O4 |
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CAS No. |
1513857-77-6 |
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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 |
3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-[(morpholin-4-yl)methyl]-1,3,4,7-tetrahydro-2Hpyrrolo[3',2':5,6]pyrido[4,3-d]pyrimidin-2-one |
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References
1. Phillip CC Liu, et al. Abstract 771: Preclinical characterization of the selective FGFR inhibitor INCB054828. AACR DOI: 10.1158/1538-7445.AM2015-771 Published August 2015.
2. Mansoor Saleh, et al. Abstract CT111: Preliminary results from a phase 1/2 study of INCB054828, a highly selective fibroblast growth factor receptor (FGFR) inhibitor, in patients with advanced malignancies. AACR DOI: 10.1158/1538-7445.AM2017-CT111 Published July 2017.
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