Infigratinib monohydrate | CAS# 1310746-11-2 | small-molecule pan-FGFR kinase inhibitor

MedKoo Cat#: 412124 | Name: Infigratinib monohydrate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Infigratinib, also known as, BGJ398 or NVP-BGJ398, is a pan FGFR kinase inhibitor, and is an orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities. pan FGFR kinase inhibitor BGJ398 selectively binds to and inhibits the activities of FGFRs, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Infigratinib was approved in 2021 to treat adults with cholangiocarcinoma whose disease meets certain criteria.

Chemical Structure

Infigratinib monohydrate

CAS#1310746-11-2 (monohydrate)

Theoretical Analysis

MedKoo Cat#: 412124

Name: Infigratinib monohydrate

CAS#: 1310746-11-2 (monohydrate)

Chemical Formula: C26H33Cl2N7O4

Exact Mass: 577.1971

Molecular Weight: 578.49

Elemental Analysis: C, 53.98; H, 5.75; Cl, 12.26; N, 16.95; O, 11.06

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

872511-34-7 (free base) 1310746-10-1 (phosphate) 1310746-11-2 (monohydrate) 1310746-12-3 (mesylate)

Synonym

Infigratinib monohydrate; BGJ-398 monohydrate; BGJ398 monohydrate; BGJ 398 monohydrate

IUPAC/Chemical Name

Urea, N'-(2,6-dichloro-3,5-dimethoxyphenyl)-N-(6-((4-(4-ethyl-1-piperazinyl)phenyl)amino)-4-pyrimidinyl)-N-methyl-, hydrate (1:1)

InChi Key

HAHRMIYGWQQRHI-UHFFFAOYSA-N

InChi Code

InChI=1S/C26H31Cl2N7O3.H2O/c1-5-34-10-12-35(13-11-34)18-8-6-17(7-9-18)31-21-15-22(30-16-29-21)33(2)26(36)32-25-23(27)19(37-3)14-20(38-4)24(25)28;/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31);1H2

SMILES Code

O=C(NC1=C(Cl)C(OC)=CC(OC)=C1Cl)N(C2=NC=NC(NC3=CC=C(N4CCN(CC)CC4)C=C3)=C2)C.[H]O[H]

Appearance

Solid powder

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

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 578.49 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

1: Tran A, Koh TS, Prawira A, Ho RZW, Le TBU, Vu TC, Hartano S, Teo XQ, Chen WC, Lee P, Thng CH, Huynh H. Dynamic Contrast-Enhanced Magnetic Resonance Imaging as Imaging Biomarker for Vascular Normalization Effect of Infigratinib in High- FGFR-Expressing Hepatocellular Carcinoma Xenografts. Mol Imaging Biol. 2020 Sep 9. doi: 10.1007/s11307-020-01531-7. Epub ahead of print. PMID: 32909245. 2: Magone MT, Hartley IR, Fitzgibbon E, Bishop R, Arango M, Moran S, Vold R, Rivero JD, Pozo K, Streit J, Roszko KL, Collins MT, Gafni RI. Ocular Adverse Effects of Infigratinib, a New Fibroblast Growth Factor Receptor Tyrosine Kinase Inhibitor. Ophthalmology. 2020 Sep 1:S0161-6420(20)30844-7. doi: 10.1016/j.ophtha.2020.08.026. Epub ahead of print. PMID: 32888946. 3: Lyou Y, Grivas P, Rosenberg JE, Hoffman-Censits J, Quinn DI, P Petrylak D, Galsky M, Vaishampayan U, De Giorgi U, Gupta S, Burris H, Rearden J, Li A, Wang H, Reyes M, Moran S, Daneshmand S, Bajorin D, Pal SK. Hyperphosphatemia Secondary to the Selective Fibroblast Growth Factor Receptor 1-3 Inhibitor Infigratinib (BGJ398) Is Associated with Antitumor Efficacy in Fibroblast Growth Factor Receptor 3-altered Advanced/Metastatic Urothelial Carcinoma. Eur Urol. 2020 Aug 23:S0302-2838(20)30616-3. doi: 10.1016/j.eururo.2020.08.002. Epub ahead of print. PMID: 32847703. 4: Makawita S, K Abou-Alfa G, Roychowdhury S, Sadeghi S, Borbath I, Goyal L, Cohn A, Lamarca A, Oh DY, Macarulla T, T Shroff R, Howland M, Li A, Cho T, Pande A, Javle M. Infigratinib in patients with advanced cholangiocarcinoma with FGFR2 gene fusions/translocations: the PROOF 301 trial. Future Oncol. 2020 Jun 25. doi: 10.2217/fon-2020-0299. Epub ahead of print. PMID: 32580579. 5: Pal SK, Bajorin D, Dizman N, Hoffman-Censits J, Quinn DI, Petrylak DP, Galsky MD, Vaishampayan U, De Giorgi U, Gupta S, Burris HA, Soifer HS, Li G, Wang H, Dambkowski CL, Moran S, Daneshmand S, Rosenberg JE. Infigratinib in upper tract urothelial carcinoma versus urothelial carcinoma of the bladder and its association with comprehensive genomic profiling and/or cell-free DNA results. Cancer. 2020 Jun 1;126(11):2597-2606. doi: 10.1002/cncr.32806. Epub 2020 Mar 24. PMID: 32208524; PMCID: PMC7515773. 6: Felix NS, de Mendonça L, Braga CL, da Silva JS, Samary CDS, Vieira JB, Cruz F, Rocha NN, Zapata-Sudo G, Rocco PRM, Silva PL. Effects of the FGF receptor-1 inhibitor, infigratinib, with or without sildenafil, in experimental pulmonary arterial hypertension. Br J Pharmacol. 2019 Dec;176(23):4462-4473. doi: 10.1111/bph.14807. Epub 2019 Dec 5. PMID: 31351013; PMCID: PMC6932937. 7: Huynh H, Lee LY, Goh KY, Ong R, Hao HX, Huang A, Wang Y, Graus Porta D, Chow P, Chung A. Infigratinib Mediates Vascular Normalization, Impairs Metastasis, and Improves Chemotherapy in Hepatocellular Carcinoma. Hepatology. 2019 Mar;69(3):943-958. doi: 10.1002/hep.30481. PMID: 30575985; PMCID: PMC6635738.