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453556 Larotrectinib (ARRY 470, LOXO 101) CAS: 1223403-58-4

Specifications
References
CAS Number
1223403-58-4
Grade
Highly Purified
Molecular Formula
C₂₁H₂₂F₂N₆O₂
Molecular Weight
428.44
EU Commodity Code
38220090
Shipping Temp
RT
Storage Temp
-20°C
(3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide; ARRY 470; LOXO 101; Vitrakvi.; (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide

A potent ATP-competitive inhibitor of tropomyosin-related kinases (TRK1, TRK2 and TRK3), members of the receptor tyrosine kinase family of neurotrophin receptors. Tumors with oncogenic TRK fusions are sensitive to larotrectinib, leading to reduced proliferation and tumor growth in patients with soft tissue sarcoma, triple-negative breast cancer and lung cancer.

Larotrectinib, also known as ARRY-470 and LOXO-101, is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC. LOXO-101 has IC50 values in the low nanomolar range for inhibition of all three TRK family members in binding and cellular assays, with 100x selectivity over other kinases, and has shown acceptable pharmaceutical properties and safety in nonclinical models. The TRK family of neurotrophin receptors, TRKA, TRKB, and TRKC (encoded by NTRK1, NTRK2, and NTRK3 genes, respectively) and their neurotrophin ligands regulate growth, differentiation and survival of neurons.
Synonyms
(3S)-N-[5-[(2R)-2-(2,5-Difluorophenyl)-1-pyrrolidinyl]pyrazolo[1,5-a]pyrimidin-3-yl]-3-hydroxy-1-pyrrolidinecarboxamide; ARRY 470; LOXO 101; Vitrakvi.; (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
CAS Number
1223403-58-4 Sulfate: 1223405-08-0
Molecular Weight
428.44
Molecular Formula
C₂₁H₂₂F₂N₆O₂
Appearance
White to off-white solid
Purity
≥98%
Solubility
Soluble in DMSO, not in water
Storage and Stability
Store at -20°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
References
1. Attia MH, Elrazaz EZ, El-Emam SZ, Taher AT, Abdel-Aziz HA, Abouzid KAM. Synthesis and in-vitro anti-proliferative evaluation of some pyrazolo[1,5-a]pyrimidines as novel larotrectinib analogs. Bioorg Chem. 2019 Nov 21:103458. doi: 10.1016/j.bioorg.2019.103458. [Epub ahead of print] PubMed PMID: 31785854.|2. Bielack SS, Cox MC, Nathrath M, Apel K, Blattmann C, Holl T, Jenewein R, Klenk U, Klothaki P, Müller-Abt P, Ortega-Lawerenz S, Reynolds M, Scheer M, Simon-Klingenstein K, Stegmaier S, Tupper R, Vokuhl C, von Kalle T. Rapid, complete and sustained tumour response to the TRK inhibitor larotrectinib in an infant with recurrent, chemotherapy-refractory infantile fibrosarcoma carrying the characteristic ETV6-NTRK3 gene fusion. Ann Oncol. 2019 Nov 1;30(Supplement_8):viii31-viii35. doi: 10.1093/annonc/mdz382. PubMed PMID: 31738425; PubMed Central PMCID: PMC6859811.|3. Schewe DM, Lenk L, Vogiatzi F, Winterberg D, Rademacher AV, Buchmann S, Henry D, Bergmann AK, Cario G, Cox MC. Larotrectinib in TRK fusion-positive pediatric B-cell acute lymphoblastic leukemia. Blood Adv. 2019 Nov 26;3(22):3499-3502. doi: 10.1182/bloodadvances.2019000700. PubMed PMID: 31725893; PubMed Central PMCID: PMC6880891.|4. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548088/ PubMed PMID: 31643418.|5. Kato S, Fujimura J, Nozaki Y, Yamaguchi S, Takagi T, Hayashi T, Saito T, Henry D, Ku N, Suehara Y. [A Case of Pediatric Soft Tissue Sarcoma with LMNA-NTRK1 Gene Fusion Treated with Larotrectinib under Single Patient Expanded Access System]. Gan To Kagaku Ryoho. 2019 Oct;46(10):1595-1597. Japanese. PubMed PMID: 31631147.|6.. Doebele, R.C., Davis, L.E., Vaishnavi, A., et al. An oncogenic NTRK fusion in a patient with soft-tissue sarcoma with response to the tropomyosin-related kinase inhibitor LOXO-101. Cancer Discov. 5(10), 1049-1057 (2015).|7. Anon.: Cancer Discovery, 6, 4 (2016)|8. Passiglia, F., et al.: Expert Opin. Investig. Drugs, 25, 385 (2016)
USBio References
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