1223403-58-4|Larotrectinib free base|(S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide|-范德生物科技公司

Larotrectinib free base

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names：
(S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
CAS号：
1223403-58-4
MDL Number：
MF(分子式)： C21H22F2N6O2 MW(分子量)： 428.44
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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询价

中文别名	Larotrectinib free base
英文别名	LOXO 101; LOXO-101; LOXO101; ARRY-470; ARRY470; ARRY 470; Larotrectinib; Vitrakvi.
CAS号	1223403-58-4
Inchi	InChI=1S/C21H22F2N6O2/c22-13-3-4-16(23)15(10-13)18-2-1-7-28(18)19-6-9-29-20(26-19)17(11-24-29)25-21(31)27-8-5-14(30)12-27/h3-4,6,9-11,14,18,30H,1-2,5,7-8,12H2,(H,25,31)/t14-,18+/m0/s1
InchiKey	NYNZQNWKBKUAII-KBXCAEBGSA-N
分子式 Formula	C21H22F2N6O2
分子量 Molecular Weight	428.44
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	Larotrectinib free base(CAS:1223403-58-4 ):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	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.
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警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[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: Walter AW, Kandula VVR, Shah N. Larotrectinib imaging response in low-grade glioma. Pediatr Blood Cancer. 2020 Jan;67(1):e28002. doi: 10.1002/pbc.28002. Epub 2019 Sep 22. PubMed PMID: 31544356.7: Federman N, McDermott R. Larotrectinib, a highly selective tropomyosin receptor kinase (TRK) inhibitor for the treatment of TRK fusion cancer. Expert Rev Clin Pharmacol. 2019 Oct;12(10):931-939. doi: 10.1080/17512433.2019.1661775. Epub 2019 Sep 10. Review. PubMed PMID: 31469968.8: Ricciuti B, Genova C, Crinò L, Libra M, Leonardi GC. Antitumor activity of larotrectinib in tumors harboring NTRK gene fusions: a short review on the current evidence. Onco Targets Ther. 2019 Apr 30;1

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