Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Pemigatinib (formerly INCB054828; INCB-054828; Pemazyre) is a novel, potent, orally bioavailable and selective FGFR inhibitor with IC50 of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. For the treatment of bile duct cancer (cholangiocarcinoma), pemigatinib has been approved as a medicine. Inhibiting FGFR1/2/3 through binding to it, INCB054828 may lead to the suppression of signal transduction pathways associated with FGFR1/2/3. When FGFR1/2/3 is overexpressed in tumor cells, this prevents their proliferation.
Targets |
FGFR1 (IC50 = 0.4 nM); FGFR2 (IC50 = 0.5 nM); FGFR3 (IC50 = 1.2 nM); FGFR4 (IC50 = 30 nM)
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ln Vitro |
Pemigatinib effectively reduces reactive astrocytes' ability to attract myeloid cells. Pemigatinib's potential to modulate FGFR may hold promise for promoting protective mechanisms in both human and murine systems and suppressing proinflammatory astrocyte responses.[2]
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ln Vivo |
Pemigatinib does not appear to have any effect on the acute EAE disease course.[2]
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Cell Assay |
Afatinib (10 μM), UNC2025 (10 μM), or pemigatinib (10 μM) were used for a 24-hour period to stimulate primary mouse astrocytes. ACM or a control medium was used to stimulate N2A neuronal cells for a full day. After being detached, primary mouse astrocytes and N2A neuronal cells were once again washed in cold 1× PBS. It was done using live/dead staining. Furthermore, annexin V–propidium iodide staining was carried out. Prior to being acquired on a 3L Cytek Northern Lights flow cytometer, cells were first rinsed and then resuspended in annexin V binding buffer. The OMIQ platform was used to analyze the flow cytometry data.
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Animal Protocol |
Female C57Bl/6J mice of experimental autoimmune encephalomyelitis (EAE) model
2.5 mg/kg i.n. |
References |
Molecular Formula |
C24H27F2N5O4
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Molecular Weight |
487.4991
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Exact Mass |
487.20
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Elemental Analysis |
C, 59.13; H, 5.58; F, 7.79; N, 14.37; O, 13.13
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CAS # |
1513857-77-6
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Related CAS # |
1513857-77-6;1513857-77-6 (HCl);
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Appearance |
Solid powder
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SMILES |
CCN1C2=C3C=C(NC3=NC=C2CN(C1=O)C4=C(C(=CC(=C4F)OC)OC)F)CN5CCOCC5
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InChi Key |
HCDMJFOHIXMBOV-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C24H27F2N5O4/c1-4-30-21-14(11-27-23-16(21)9-15(28-23)13-29-5-7-35-8-6-29)12-31(24(30)32)22-19(25)17(33-2)10-18(34-3)20(22)26/h9-11H,4-8,12-13H2,1-3H3,(H,27,28)
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Chemical Name |
11-(2,6-difluoro-3,5-dimethoxyphenyl)-13-ethyl-4-(morpholin-4-ylmethyl)-5,7,11,13-tetrazatricyclo[7.4.0.02,6]trideca-1,3,6,8-tetraen-12-one
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Synonyms |
INCB054828; INCB54828; INCB-054828; INCB 054828; INCB 54828; INCB-54828
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 25~40 mg/mL (51.3~82.1 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (5.64 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.27 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.27 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: (saturation unknown) in (add these co-solvents sequentially from left to right, and one by one), |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.0513 mL | 10.2564 mL | 20.5128 mL | |
5 mM | 0.4103 mL | 2.0513 mL | 4.1026 mL | |
10 mM | 0.2051 mL | 1.0256 mL | 2.0513 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT04591431 | Active Recruiting |
Drug: Erlotinib Drug: Pemigatinib |
Breast Cancer Other Cancer |
Fondazione per la Medicina Personalizzata |
October 7, 2020 | Phase 2 |
NCT04096417 | Active Recruiting |
Other: Quality-of-Life Assessment Drug: Pemigatinib |
FGFR3 Gene Mutation FGFR2 Gene Mutation |
Academic and Community Cancer Research United |
August 31, 2020 | Phase 2 |
NCT04256980 | Active Recruiting |
Drug: Pemigatinib | Cholangiocarcinoma | Innovent Biologics (Suzhou) Co. Ltd. |
March 3, 2020 | Phase 2 |
NCT03011372 | Active Recruiting |
Drug: Pemigatinib | MPN (Myeloproliferative Neoplasms) |
Incyte Corporation | April 25, 2017 | Phase 2 |
NCT04949191 | Completed | Drug: Pemigatinib Drug: Retifanlimab |
Advanced Malignancies | Incyte Corporation | July 12, 2021 | Phase 2 |
Therapeutic potential of i.n. afatinib and pemigatinib application in acute EAE. JCI Insight . 2022 Apr 8;7(7):e154824. td> |
Schematic mechanism of action of afatinib, UNC2025, and pemigatinib. JCI Insight . 2022 Apr 8;7(7):e154824. td> |