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MedKoo Cat#: 584684 | Name: GUN55146

Description:

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

GUN55146, also known as RET-​IN-​1, is an oral and selective investigational drug in clinical development for the treatment of patients with cancers that harbor abnormalities in the rearranged during transfection (RET) kinase. GUN55146 was previously mistakenly list as LOXO-292 (ARRY-192 or Selpercatinib). This product has no formal name at the moment. For the convenience of communication, a temporary code name was therefore proposed according to MedKoo Chemical Nomenclature (see web page: https://www.medkoo.com/page/naming).

Chemical Structure

GUN55146
GUN55146
CAS#2222755-14-6

Theoretical Analysis

MedKoo Cat#: 584684

Name: GUN55146

CAS#: 2222755-14-6

Chemical Formula: C29H31N9O3

Exact Mass: 553.2550

Molecular Weight: 553.63

Elemental Analysis: C, 62.92; H, 5.64; N, 22.77; O, 8.67

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 #
No Data
Synonym
RET-​IN-​1; GUN55146; GUN-55146; GUN 55146; LOXO-292; LOXO292; LOXO 292; ARRY-192; ARRY192; ARRY 192;
IUPAC/Chemical Name
4-(5-(6-((6-methoxypyridin-3-yl)methyl)-3,6-diazabicyclo[3.1.1]heptan-3-yl)pyrazin-2-yl)-6-(((R)-morpholin-2-yl)methoxy)pyrazolo[1,5-a]pyridine-3-carbonitrile
InChi Key
GTQISTQEBXXLPC-UBVWURDFSA-N
InChi Code
InChI=1S/C29H31N9O3/c1-39-28-3-2-19(9-34-28)14-37-21-6-22(37)16-36(15-21)27-13-32-26(12-33-27)25-7-23(41-18-24-11-31-4-5-40-24)17-38-29(25)20(8-30)10-35-38/h2-3,7,9-10,12-13,17,21-22,24,31H,4-6,11,14-16,18H2,1H3/t21?,22?,24-/m1/s1
SMILES Code
N#CC1=C2C(C3=NC=C(N4CC(C5)N(CC6=CC=C(OC)N=C6)C5C4)N=C3)=CC(OC[C@H]7CNCCO7)=CN2N=C1
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
Solvent mg/mL mM
Solubility
Soluble in DMSO 0.0 0.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 553.63 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
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.

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GUN81846

GUN81846