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2020年11月1日星期日

Selpercatinib | LOXO-292 | CAS:2152628-33-4 | RET inhibitor | Eos Med Chem

Selpercatinib Manufacturer and Supplier

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EOS Med Chem is a pharmaceutical manufacturer specialisting in Selpercatinib (LOXO-292) and many other medical substance. Thanks to our production ability, we can supply all type of quantity orders. 

We are pround that we are one of the very few manufacturers in the world who has GMP (Good Manufacturing Practice) production lines. 

We are also ISO-9001 certified and following Drug Master File (DMF) guidelines.

Here is our pricing list for Selpercatinib (LOXO-292).

SELPERCATINIB / LOXO-292 PRICE AND AVAILABILITY

SizeUnit PricePriceShipping
1 gUSD 980 / gUSD 9801 - 2 Weeks
10 gUSD 550 / gUSD 5,5001 - 2 Weeks
50 gUSD 350 / gUSD 17,5001 - 2 Weeks
100 gUSD 190 / gUSD 19,5001 - 2 Weeks

EMAIL: info@eosmedchem.com / TEL: 0086-531-69905422 

CAS No.: 2152628-33-4 

Description: Selpercatinib, also known as LOXO-292, is a potent and selective RET inhibitor with antineoplastic properties. LOXO-292 selectively binds to and targets various RET mutants and RET-containing fusion products. This results in an inhibition of cell growth of tumors cells that exhibit increased RET activity. Selpercatinib was approved in May 2020.

SELPERCATINIB / LOXO-292 THEORETICAL ANALYSIS

Name: Selpercatinib
CAS No.: 2152628-33-4
Chemical Formula: C29H31N7O3
Exact Mass: 525.2488
Molecular Weight: 525.613
Elemental Analysis: C, 66.27; H, 5.95; N, 18.65; O, 9.13





SELPERCATINIB / LOXO-292 DETAILS

Related CAS No.: 2152628-33-4    2306313-13-1 (HCl)   2306313-14-2 (sulfate)   2306313-16-4 (tosylate)   2306313-17-5 (mesylate)   2306313-19-7 (besylate)   2306313-23-3 (maleate)   2306313-28-8 (fumarate)   2306313-27-7 (tartrate)   2306313-29-9 (citrate)  

Synonym: LOXO-292; LOXO292; LOXO 292; ARRY-192; ARRY192; ARRY 192; Selpercatinib;

IUPAC/Chemical Name: 6-(2-hydroxy-2-methylpropoxy)-4-(6-{6-[(6-methoxypyridin-3-yl)methyl]-3,6-diazabicyclo[3.1.1]heptan-3-yl}pyridin-3- yl)pyrazolo[1,5-a]pyridine-3-carbonitrile

InChi Key: XIIOFHFUYBLOLW-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H31N7O3/c1-29(2,37)18-39-24-9-25(28-21(10-30)13-33-36(28)17-24)20-5-6-26(31-12-20)34-15-22-8-23(16-34)35(22)14-19-4-7-27(38-3)32-11-19/h4-7,9,11-13,17,22-23,37H,8,14-16,18H2,1-3H3

SMILES Code: N#CC1=C2C(C3=CC=C(N4CC(C5)N(CC6=CC=C(OC)N=C6)C5C4)N=C3)=CC(OCC(C)(O)C)=CN2N=C1


SELPERCATINIB / LOXO-292 TECHNICAL DATA

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


ADDITIONAL INFORMATION on SELPERCATINIB / LOXO-292

RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers.


REFERENCES

1: Russo A, Lopes AR, McCusker MG, Garrigues SG, Ricciardi GR, Arensmeyer KE, Scilla KA, Mehra R, Rolfo C. New Targets in Lung Cancer (Excluding EGFR, ALK, ROS1). Curr Oncol Rep. 2020 Apr 16;22(5):48. doi: 10.1007/s11912-020-00909-8. PMID: 32296961.

2: Dias-Santagata D, Lennerz JK, Sadow PM, Frazier RP, Govinda Raju S, Henry D, Chung T, Kherani J, Rothenberg SM, Wirth LJ. Response to RET-Specific Therapy in RET Fusion-Positive Anaplastic Thyroid Carcinoma. Thyroid. 2020 Apr 15. doi: 10.1089/thy.2019.0477. Epub ahead of print. PMID: 32292131.

3: Zhao Z, Fu T, Gao J, Xu Y, Wu X, Chen W, Li X, Yu R, Shao YW, Li M, Yao Y. Identifying novel oncogenic RET mutations and characterising their sensitivity to RET-specific inhibitors. J Med Genet. 2020 Apr 13:jmedgenet-2019-106546. doi: 10.1136/jmedgenet-2019-106546. Epub ahead of print. PMID: 32284345.

4: Solomon BJ, Tan L, Lin JJ, Wong SQ, Hollizeck S, Ebata K, Tuch BB, Yoda S, Gainor JF, Sequist LV, Oxnard GR, Gautschi O, Drilon A, Subbiah V, Khoo C, Zhu EY, Nguyen M, Henry D, Condroski KR, Kolakowski GR, Gomez E, Ballard J, Metcalf AT, Blake JF, Dawson SJ, Blosser W, Stancato LF, Brandhuber BJ, Andrews S, Robinson BG, Rothenberg SM. RET Solvent Front Mutations Mediate Acquired Resistance to Selective RET Inhibition in RET-Driven Malignancies. J Thorac Oncol. 2020 Apr;15(4):541-549. doi: 10.1016/j.jtho.2020.01.006. Epub 2020 Jan 24. PMID: 31988000.

5: Tiedje V, Fagin JA. Therapeutic breakthroughs for metastatic thyroid cancer. Nat Rev Endocrinol. 2020 Feb;16(2):77-78. doi: 10.1038/s41574-019-0307-2. PMID: 31819229.

6: Durham BH, Lopez Rodrigo E, Picarsic J, Abramson D, Rotemberg V, De Munck S, Pannecoucke E, Lu SX, Pastore A, Yoshimi A, Mandelker D, Ceyhan-Birsoy O, Ulaner GA, Walsh M, Yabe M, Petrova-Drus K, Arcila ME, Ladanyi M, Solit DB, Berger MF, Hyman DM, Lacouture ME, Erickson C, Saganty R, Ki M, Dunkel IJ, Santa-María López V, Mora J, Haroche J, Emile JF, Decaux O, Geissmann F, Savvides SN, Drilon A, Diamond EL, Abdel-Wahab O. Activating mutations in CSF1R and additional receptor tyrosine kinases in histiocytic neoplasms. Nat Med. 2019 Dec;25(12):1839-1842. doi: 10.1038/s41591-019-0653-6. Epub 2019 Nov 25. PMID: 31768065; PMCID: PMC6898787.

7: Li AY, McCusker MG, Russo A, Scilla KA, Gittens A, Arensmeyer K, Mehra R, Adamo V, Rolfo C. RET fusions in solid tumors. Cancer Treat Rev. 2019 Dec;81:101911. doi: 10.1016/j.ctrv.2019.101911. Epub 2019 Oct 30. PMID: 31715421.

8: Hillier K, Hughes A, Shamberger RC, Shusterman S, Perez-Atayde AR, Wassner AJ, Iafrate AJ, Dubuc A, Janeway KA, Rothenberg SM, Cox MC, Randolph GW, Wirth LJ, Tsai H, Church A, DuBois SG. A Novel ALK Fusion in Pediatric Medullary Thyroid Carcinoma. Thyroid. 2019 Nov;29(11):1704-1707. doi: 10.1089/thy.2019.0041. PMID: 31650892.

9: Ackermann CJ, Stock G, Tay R, Dawod M, Gomes F, Califano R. Targeted Therapy For RET-Rearranged Non-Small Cell Lung Cancer: Clinical Development And Future Directions. Onco Targets Ther. 2019 Sep 24;12:7857-7864. doi: 10.2147/OTT.S171665. PMID: 31576143; PMCID: PMC6767757.

10: Guo R, Schreyer M, Chang JC, Rothenberg SM, Henry D, Cotzia P, Kris MG, Rekhtman N, Young RJ, Hyman DM, Drilon A. Response to Selective RET Inhibition With LOXO-292 in a Patient With RET Fusion-Positive Lung Cancer With Leptomeningeal Metastases. JCO Precis Oncol. 2019;3:10.1200/PO.19.00021. doi: 10.1200/PO.19.00021. Epub 2019 Jun 3. PMID: 31485557; PMCID: PMC6724540.

11: O'Leary C, Xu W, Pavlakis N, Richard D, O'Byrne K. Rearranged During Transfection Fusions in Non-Small Cell Lung Cancer. Cancers (Basel). 2019 May 3;11(5):620. doi: 10.3390/cancers11050620. PMID: 31058838; PMCID: PMC6562639.

12: Bronte G, Ulivi P, Verlicchi A, Cravero P, Delmonte A, Crinò L. Targeting RET-rearranged non-small-cell lung cancer: future prospects. Lung Cancer (Auckl). 2019 Mar 20;10:27-36. doi: 10.2147/LCTT.S192830. PMID: 30962732; PMCID: PMC6433115.

13: Subbiah V, Velcheti V, Tuch BB, Ebata K, Busaidy NL, Cabanillas ME, Wirth LJ, Stock S, Smith S, Lauriault V, Corsi-Travali S, Henry D, Burkard M, Hamor R, Bouhana K, Winski S, Wallace RD, Hartley D, Rhodes S, Reddy M, Brandhuber BJ, Andrews S, Rothenberg SM, Drilon A. Selective RET kinase inhibition for patients with RET-altered cancers. Ann Oncol. 2018 Aug 1;29(8):1869-1876. doi: 10.1093/annonc/mdy137. PMID: 29912274; PMCID: PMC6096733.

14: LOXO-292 Reins In RET-Driven Tumors. Cancer Discov. 2018 Aug;8(8):904-905. doi: 10.1158/2159-8290.CD-NB2018-070. Epub 2018 Jun 2. PMID: 29860229.

15: Sabari JK, Siau ED, Drilon A. Targeting RET-rearranged lung cancers with multikinase inhibitors. Oncoscience. 2017 Apr 14;4(3-4):23-24. doi: 10.18632/oncoscience.345. PMID: 28540330; PMCID: PMC5441470.

EMAIL: info@eosmedchem.com / TEL: 0086-531-69905422