WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H140244
CAS#: 2750709-91-0
Description: Resigratinib, also known as KIN-3248, is a fibroblast growth factor receptor tyrosine kinase inhibitor and antineoplastic. KIN-3248 is active against many acquired resistance mutations.
Hodoodo Cat#: H140244
Name: Resigratinib
CAS#: 2750709-91-0
Chemical Formula: C26H27F2N7O3
Exact Mass: 523.21
Molecular Weight: 523.545
Elemental Analysis: C, 59.65; H, 5.20; F, 7.26; N, 18.73; O, 9.17
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Synonym: Resigratinib; KIN-3248; KIN 3248; KIN3248;
IUPAC/Chemical Name: 1-((3S,5R)-1-acryloyl-5-(methoxymethyl)pyrrolidin-3-yl)-3-((1-cyclopropyl-4,6-difluoro-1H-benzo[d]imidazol-5-yl)ethynyl)-5-(methylamino)-1H-pyrazole-4-carboxamide
InChi Key: YXVDEILMUVTDMK-JKSUJKDBSA-N
InChi Code: InChI=1S/C26H27F2N7O3/c1-4-21(36)33-11-15(9-16(33)12-38-3)35-26(30-2)22(25(29)37)19(32-35)8-7-17-18(27)10-20-24(23(17)28)31-13-34(20)14-5-6-14/h4,10,13-16,30H,1,5-6,9,11-12H2,2-3H3,(H2,29,37)/t15-,16+/m0/s1
SMILES Code: NC(C1=C(NC)N([C@]2([H])CN(C(C=C)=O)[C@](COC)([H])C2)N=C1C#CC3=C(F)C(N=CN4C5CC5)=C4C=C3F)=O
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info: Fibroblast growth factor receptor (FGFR) alterations are present as oncogenic drivers and bypass mechanisms in many forms of cancer. These alterations can include fusions, amplifications, rearrangements, and mutations. Acquired drug resistance to current FGFR inhibitors often results in disease progression and unfavorable outcomes for patients. Genomic profiling of tumors refractory to current FGFR inhibitors in the clinic has revealed several acquired driver alterations that could be the target of next generation therapeutics.
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In vivo activity: |
The following data is based on the product molecular weight 523.54 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
Tyhonas JS, Arnold LD, Cox JM, Franovic A, Gardiner E, Grandinetti K, Kania R, Kanouni T, Lardy M, Li C, Martin ES, Miller N, Mohan A, Murphy EA, Perez M, Soroceanu L, Timple N, Uryu S, Womble S, Kaldor SW. Discovery of KIN-3248, An Irreversible, Next Generation FGFR Inhibitor for the Treatment of Advanced Tumors Harboring FGFR2 and/or FGFR3 Gene Alterations. J Med Chem. 2024 Feb 8;67(3):1734-1746. doi: 10.1021/acs.jmedchem.3c01819. Epub 2024 Jan 24. PMID: 38267212.