Infigratinib phosphate
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MedKoo CAT#: 206947

CAS#: 1310746-10-1 (phosphate)

Description: 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

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Infigratinib phosphate
CAS# 1310746-10-1 (phosphate)

Theoretical Analysis

MedKoo Cat#: 206947
Name: Infigratinib phosphate
CAS#: 1310746-10-1 (phosphate)
Chemical Formula: C26H34Cl2N7O7P
Exact Mass: 0.00
Molecular Weight: 658.474
Elemental Analysis: C, 47.43; H, 5.20; Cl, 10.77; N, 14.89; O, 17.01; P, 4.70

Price and Availability

Size Price Availability Quantity
10mg USD 275 2 Weeks
50mg USD 550 2 Weeks
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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 phosphate; NVPBGJ398; NVPBGJ 398; NVPBGJ-398; BGJ398; BGJ-398; BG J398; Infigratinib.

IUPAC/Chemical Name: 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-(6-((4-(4-ethylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)-1-methylurea phosphate

InChi Key: GUQNHCGYHLSITB-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H31Cl2N7O3.H3O4P/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;1-5(2,3)4/h6-9,14-16H,5,10-13H2,1-4H3,(H,32,36)(H,29,30,31);(H3,1,2,3,4)

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.O=P(O)(O)O

Appearance: White to off-white 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: >2 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:

Product Data:
Biological target: Infigratinib phosphate (BGJ-398 phosphate; NVP-BGJ398 phosphate) is a potent inhibitor of the FGFR family with IC50 of 0.9 nM, 1.4 nM, 1 nM, and 60 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
In vitro activity: Infigratinib inhibits FGF-induced activation of the FGFR signaling pathway and cell cycle progression. Pretreatment of HCC01-0909 cells with 1.0 µM Infigratinib for 18 hours abolished FGF-2-, FGF-1-, and FGF-19- stimulated phosphorylation of Fibroblast Growth Factor Receptor Substrate 2 alpha (FRS2-α) and extracellular signal-regulated kinase (ERK)1/2 (Fig. 1C). Infigratinib had no effect on HGF-induced phosphorylation of ERK1/2, suggesting that the inhibitory effect of infigratinib was specific to the FGF/FGFR signaling pathway. Infigratinib caused a significant increase in the percentage of cells in the G1 and sub-G1 phases with a concomitant reduction in the percentage of cells in the G2/M and S phases (Fig. 1D), suggesting that infigratinib causes G1 cell cycle arrest. Reference: Hepatology. 2019 Mar;69(3):943-958. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6635738/
In vivo activity: Daily treatment of HCC06-0606 tumor-bearing mice with 10, 20, and 30 mg/kg infigratinib for 14 days led to approximately 65%, 96%, and 98% reductions in tumor burden, respectively (Fig. 1E). Daily treatment of mice with infigratinib resulted in significant elevation in alanine aminotransferase (ALT), alkaline phosphatase (ALP), and aspartate aminotransferase (AST) and a significant decrease in serum creatinine (Supporting Fig. S2). Infigratinib potently inhibited p-FRS2-α and p-ERK1/2 (Figure 1F), and the inhibition of these biomarkers occurred within 2 hours after a single oral dose of 20 mg/kg infigratinib, was maintained for approximately 10 hours, and returned to baseline by 12 hours after treatment (Fig. 2A). Reference: Hepatology. 2019 Mar;69(3):943-958. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6635738/

Preparing Stock Solutions

The following data is based on the product molecular weight 658.47 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.

Recalculate based on batch purity %
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: 1. 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.
In vitro protocol: 1. 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.
In vivo protocol: 1. 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.

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1: Sahores A, May M, Sequeira G, Fuentes C, Jacobsen B, Lanari C, Lamb CA. Targeting FGFR with BGJ398 in breast cancer: Effect on tumor growth and metastasis. Curr Cancer Drug Targets. 2017 Dec 13. doi: 10.2174/1568009618666171214114706. [Epub ahead of print] PubMed PMID: 29237381.

2: Gilbert JA. BGJ398 for FGFR-altered advanced cholangiocarcinoma. Lancet Oncol. 2018 Jan;19(1):e16. doi: 10.1016/S1470-2045(17)30902-6. Epub 2017 Dec 7. PubMed PMID: 29233557.

3: Takamura T, Horinaka M, Yasuda S, Toriyama S, Aono Y, Sowa Y, Miki T, Ukimura O, Sakai T. FGFR inhibitor BGJ398 and HDAC inhibitor OBP-801 synergistically inhibit cell growth and induce apoptosis in bladder cancer cells. Oncol Rep. 2018 Feb;39(2):627-632. doi: 10.3892/or.2017.6127. Epub 2017 Dec 1. PubMed PMID: 29207153.

4: Javle M, Lowery M, Shroff RT, Weiss KH, Springfeld C, Borad MJ, Ramanathan RK, Goyal L, Sadeghi S, Macarulla T, El-Khoueiry A, Kelley RK, Borbath I, Choo SP, Oh DY, Philip PA, Chen LT, Reungwetwattana T, Van Cutsem E, Yeh KH, Ciombor K, Finn RS, Patel A, Sen S, Porter D, Isaacs R, Zhu AX, Abou-Alfa GK, Bekaii-Saab T. Phase II Study of BGJ398 in Patients With FGFR-Altered Advanced Cholangiocarcinoma. J Clin Oncol. 2018 Jan 20;36(3):276-282. doi: 10.1200/JCO.2017.75.5009. Epub 2017 Nov 28. PubMed PMID: 29182496.

5: Cha HJ, Choi JH, Park IC, Kim CH, An SK, Kim TJ, Lee JH. Selective FGFR inhibitor BGJ398 inhibits phosphorylation of AKT and STAT3 and induces cytotoxicity in sphere-cultured ovarian cancer cells. Int J Oncol. 2017 Mar 15. doi: 10.3892/ijo.2017.3913. [Epub ahead of print] PubMed PMID: 28350116.

6: Datta J, Damodaran S, Parks H, Ocrainiciuc C, Miya J, Yu L, Gardner EP, Samorodnitsky E, Wing MR, Bhatt D, Hays J, Reeser JW, Roychowdhury S. Akt Activation Mediates Acquired Resistance to Fibroblast Growth Factor Receptor Inhibitor BGJ398. Mol Cancer Ther. 2017 Apr;16(4):614-624. doi: 10.1158/1535-7163.MCT-15-1010. Epub 2017 Mar 2. PubMed PMID: 28255027; PubMed Central PMCID: PMC5539948.

7: Nogova L, Sequist LV, Perez Garcia JM, Andre F, Delord JP, Hidalgo M, Schellens JH, Cassier PA, Camidge DR, Schuler M, Vaishampayan U, Burris H, Tian GG, Campone M, Wainberg ZA, Lim WT, LoRusso P, Shapiro GI, Parker K, Chen X, Choudhury S, Ringeisen F, Graus-Porta D, Porter D, Isaacs R, Buettner R, Wolf J. Evaluation of BGJ398, a Fibroblast Growth Factor Receptor 1-3 Kinase Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in Fibroblast Growth Factor Receptors: Results of a Global Phase I, Dose-Escalation and Dose-Expansion Study. J Clin Oncol. 2017 Jan 10;35(2):157-165. Epub 2016 Nov 21. PubMed PMID: 27870574.

8: Komla-Ebri D, Dambroise E, Kramer I, Benoist-Lasselin C, Kaci N, Le Gall C, Martin L, Busca P, Barbault F, Graus-Porta D, Munnich A, Kneissel M, Di Rocco F, Biosse-Duplan M, Legeai-Mallet L. Tyrosine kinase inhibitor NVP-BGJ398 functionally improves FGFR3-related dwarfism in mouse model. J Clin Invest. 2016 May 2;126(5):1871-84. doi: 10.1172/JCI83926. Epub 2016 Apr 11. PubMed PMID: 27064282; PubMed Central PMCID: PMC4855917.

9: Schmidt K, Moser C, Hellerbrand C, Zieker D, Wagner C, Redekopf J, Schlitt HJ, Geissler EK, Lang SA. Targeting Fibroblast Growth Factor Receptor (FGFR) with BGJ398 in a Gastric Cancer Model. Anticancer Res. 2015 Dec;35(12):6655-65. PubMed PMID: 26637881.

10: Göke A, Göke R, Ofner A, Herbst A, Lankat-Buttgereit B. The FGFR Inhibitor NVP-BGJ398 Induces NSCLC Cell Death by Activating Caspase-dependent Pathways as well as Caspase-independent Apoptosis. Anticancer Res. 2015 Nov;35(11):5873-9. PubMed PMID: 26504010.

11: Gudernova I, Vesela I, Balek L, Buchtova M, Dosedelova H, Kunova M, Pivnicka J, Jelinkova I, Roubalova L, Kozubik A, Krejci P. Multikinase activity of fibroblast growth factor receptor (FGFR) inhibitors SU5402, PD173074, AZD1480, AZD4547 and BGJ398 compromises the use of small chemicals targeting FGFR catalytic activity for therapy of short-stature syndromes. Hum Mol Genet. 2016 Jan 1;25(1):9-23. doi: 10.1093/hmg/ddv441. Epub 2015 Oct 22. PubMed PMID: 26494904.

12: Göke F, Franzen A, Hinz TK, Marek LA, Yoon P, Sharma R, Bode M, von Maessenhausen A, Lankat-Buttgereit B, Göke A, Golletz C, Kirsten R, Boehm D, Vogel W, Kleczko EK, Eagles JR, Hirsch FR, Van Bremen T, Bootz F, Schroeck A, Kim J, Tan AC, Jimeno A, Heasley LE, Perner S. FGFR1 Expression Levels Predict BGJ398 Sensitivity of FGFR1-Dependent Head and Neck Squamous Cell Cancers. Clin Cancer Res. 2015 Oct 1;21(19):4356-64. doi: 10.1158/1078-0432.CCR-14-3357. Epub 2015 May 26. PubMed PMID: 26015511; PubMed Central PMCID: PMC4592392.

13: Konecny GE, Kolarova T, O'Brien NA, Winterhoff B, Yang G, Qi J, Qi Z, Venkatesan N, Ayala R, Luo T, Finn RS, Kristof J, Galderisi C, Porta DG, Anderson L, Shi MM, Yovine A, Slamon DJ. Activity of the fibroblast growth factor receptor inhibitors dovitinib (TKI258) and NVP-BGJ398 in human endometrial cancer cells. Mol Cancer Ther. 2013 May;12(5):632-42. doi: 10.1158/1535-7163.MCT-12-0999. Epub 2013 Feb 26. PubMed PMID: 23443805.

14: Guagnano V, Kauffmann A, Wöhrle S, Stamm C, Ito M, Barys L, Pornon A, Yao Y, Li F, Zhang Y, Chen Z, Wilson CJ, Bordas V, Le Douget M, Gaither LA, Borawski J, Monahan JE, Venkatesan K, Brümmendorf T, Thomas DM, Garcia-Echeverria C, Hofmann F, Sellers WR, Graus-Porta D. FGFR genetic alterations predict for sensitivity to NVP-BGJ398, a selective pan-FGFR inhibitor. Cancer Discov. 2012 Dec;2(12):1118-33. doi: 10.1158/2159-8290.CD-12-0210. Epub 2012 Sep 20. PubMed PMID: 23002168.

15: Guagnano V, Furet P, Spanka C, Bordas V, Le Douget M, Stamm C, Brueggen J, Jensen MR, Schnell C, Schmid H, Wartmann M, Berghausen J, Drueckes P, Zimmerlin A, Bussiere D, Murray J, Graus Porta D. Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamin o]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem. 2011 Oct 27;54(20):7066-83. doi: 10.1021/jm2006222. Epub 2011 Sep 21. PubMed PMID: 21936542.