SU12662 | CAS#356068-97-8 | RTK inhibitor

MedKoo Cat#: 465385 | Name: SU12662

Description:

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

SU12662 is a RTK inhibitor and the N-dealkylation product of sunitinib. SU12662 exhibited comparable in vitro and in vivo properties.

Chemical Structure

SU12662

CAS#356068-97-8

Theoretical Analysis

MedKoo Cat#: 465385

Name: SU12662

CAS#: 356068-97-8

Chemical Formula: C20H23FN4O2

Exact Mass: 370.1805

Molecular Weight: 370.43

Elemental Analysis: C, 64.85; H, 6.26; F, 5.13; N, 15.13; O, 8.64

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.

Bulk Inquiry

Related CAS #

No Data

Synonym

SU12662; SU 12662; SU-12662; N-Desethyl Sunitinib

IUPAC/Chemical Name

(Z)-N-(2-(ethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide

InChi Key

LIZNIAKSBJKPQC-GDNBJRDFSA-N

InChi Code

InChI=1S/C20H23FN4O2/c1-4-22-7-8-23-20(27)18-11(2)17(24-12(18)3)10-15-14-9-13(21)5-6-16(14)25-19(15)26/h5-6,9-10,22,24H,4,7-8H2,1-3H3,(H,23,27)(H,25,26)/b15-10-

SMILES Code

O=C(NCCN([H])CC)C1=C(C)NC(/C=C(C2=CC(F)=CC=C2N3)\C3=O)=C1C

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 370.43 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.

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: Yu Y, DuBois SG, Wetmore C, Khosravan R. Physiologically Based Pharmacokinetic Modeling and Simulation of Sunitinib in Pediatrics. AAPS J. 2020 Jan 23;22(2):31. doi: 10.1208/s12248-020-0423-x. PMID: 31975150. 2: Gurjar M, Mehta P, Sharma J, Patil S, Kulkarni P, Patil A, Nookala M, Joshi A, Gota V. An HPLC method for simultaneous quantification of sunitinib and its active metabolite, SU12662, using hydrophilic interaction chromatography principle. Bioanalysis. 2020 Jan;12(2):75-85. doi: 10.4155/bio-2019-0188. PMID: 31928228. 3: Marangon E, Buzzo M, Posocco B, Gagno S, Zanchetta M, Iacuzzi V, Poetto AS, Guardascione M, Giodini L, Toffoli G. A new high-performance liquid chromatography-tandem mass spectrometry method for the determination of sunitinib and N-desethyl sunitinib in human plasma: Light-induced isomerism overtaking towards therapeutic drug monitoring in clinical routine. J Pharm Biomed Anal. 2020 Feb 5;179:112949. doi: 10.1016/j.jpba.2019.112949. Epub 2019 Oct 25. PMID: 31784210. 4: Matsunaga N, Kitahara T, Yamada M, Sato K, Kodama Y, Sasaki H. The influence of light sources on sunitinib measurements with photoisomerization. Biomed Chromatogr. 2019 Feb;33(2):e4407. doi: 10.1002/bmc.4407. Epub 2018 Nov 8. PMID: 30315654. 5: Posocco B, Buzzo M, Giodini L, Crotti S, D'Aronco S, Traldi P, Agostini M, Marangon E, Toffoli G. Analytical aspects of sunitinib and its geometric isomerism towards therapeutic drug monitoring in clinical routine. J Pharm Biomed Anal. 2018 Oct 25;160:360-367. doi: 10.1016/j.jpba.2018.08.013. Epub 2018 Aug 8. PMID: 30119000. 6: Pellat A, Dreyer C, Couffignal C, Walter T, Lombard-Bohas C, Niccoli P, Seitz JF, Hentic O, André T, Coriat R, Faivre S, Zappa M, Ruszniewski P, Pote N, Couvelard A, Raymond E. Clinical and Biomarker Evaluations of Sunitinib in Patients with Grade 3 Digestive Neuroendocrine Neoplasms. Neuroendocrinology. 2018;107(1):24-31. doi: 10.1159/000487237. Epub 2018 Mar 8. PMID: 29518779. 7: Fuchs K, Kiss A, Bize PE, Duran R, Denys A, Hopfgartner G, Borchard G, Jordan O. Mapping of drug distribution in the rabbit liver tumor model by complementary fluorescence and mass spectrometry imaging. J Control Release. 2018 Jan 10;269:128-135. doi: 10.1016/j.jconrel.2017.10.042. Epub 2017 Oct 31. PMID: 29101054. 8: Cabel L, Blanchet B, Thomas-Schoemann A, Huillard O, Bellesoeur A, Cessot A, Giroux J, Boudou-Rouquette P, Coriat R, Vidal M, Saidu NEB, Golmard L, Alexandre J, Goldwasser F. Drug monitoring of sunitinib in patients with advanced solid tumors: a monocentric observational French study. Fundam Clin Pharmacol. 2018 Feb;32(1):98-107. doi: 10.1111/fcp.12327. Epub 2017 Nov 10. PMID: 29055166. 9: Diekstra MH, Fritsch A, Kanefendt F, Swen JJ, Moes D, Sörgel F, Kinzig M, Stelzer C, Schindele D, Gauler T, Hauser S, Houtsma D, Roessler M, Moritz B, Mross K, Bergmann L, Oosterwijk E, Kiemeney LA, Guchelaar HJ, Jaehde U. Population Modeling Integrating Pharmacokinetics, Pharmacodynamics, Pharmacogenetics, and Clinical Outcome in Patients With Sunitinib-Treated Cancer. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):604-613. doi: 10.1002/psp4.12210. Epub 2017 Jul 13. PMID: 28571114; PMCID: PMC5613186. 10: Noé G, Bellesoeur A, Thomas-Schoemann A, Rangarajan S, Naji F, Puszkiel A, Huillard O, Saidu N, Golmard L, Alexandre J, Goldwasser F, Blanchet B, Vidal M. Clinical and kinomic analysis identifies peripheral blood mononuclear cells as a potential pharmacodynamic biomarker in metastatic renal cell carcinoma patients treated with sunitinib. Oncotarget. 2016 Oct 11;7(41):67507-67520. doi: 10.18632/oncotarget.11686. PMID: 27589830; PMCID: PMC5341893. 11: Chae JW, Teo YL, Ho HK, Lee J, Back HM, Yun HY, Karlsson MO, Kwon KI, Chan A. BSA and ABCB1 polymorphism affect the pharmacokinetics of sunitinib and its active metabolite in Asian mRCC patients receiving an attenuated sunitinib dosing regimen. Cancer Chemother Pharmacol. 2016 Sep;78(3):623-32. doi: 10.1007/s00280-016-3104-9. Epub 2016 Aug 2. PMID: 27485537. 12: Sobańska K, Karbownik A, Szałek E, Płotek W, Grabowski T, Szewczyk A, Marcinkowska D, Połom W, Matuszewski M, Grześkowiak E. The influence of the time-of-day administration of sunitinib on the penetration through the blood- brain and blood-aqueous humour barriers in rabbits. Eur Rev Med Pharmacol Sci. 2016;20(1):166-73. PMID: 26813470. 13: Takayoshi K, Sagara K, Uchino K, Kusaba H, Sakamoto N, Iguchi A, Baba E. A case of metastatic renal cell carcinoma and bile duct carcinoma treated with a combination of sunitinib and gemcitabine. BMC Cancer. 2015 May 22;15:426. doi: 10.1186/s12885-015-1443-2. PMID: 26001650; PMCID: PMC4491890. 14: Rodríguez J, Castañeda G, Muñoz L, Villa JC. Quantitation of sunitinib, an oral multitarget tyrosine kinase inhibitor, and its metabolite in urine samples by nonaqueous capillary electrophoresis time of flight mass spectrometry. Electrophoresis. 2015 Jul;36(14):1580-7. doi: 10.1002/elps.201400588. Epub 2015 May 20. PMID: 25873554. 15: Teo YL, Wee HL, Chue XP, Chau NM, Tan MH, Kanesvaran R, Wee HL, Ho HK, Chan A. Effect of the CYP3A5 and ABCB1 genotype on exposure, clinical response and manifestation of toxicities from sunitinib in Asian patients. Pharmacogenomics J. 2016 Feb;16(1):47-53. doi: 10.1038/tpj.2015.13. Epub 2015 Mar 17. PMID: 25778465. 16: Kloth JS, Binkhorst L, de Wit AS, de Bruijn P, Hamberg P, Lam MH, Burger H, Chaves I, Wiemer EA, van der Horst GT, Mathijssen RH. Relationship Between Sunitinib Pharmacokinetics and Administration Time: Preclinical and Clinical Evidence. Clin Pharmacokinet. 2015 Aug;54(8):851-8. doi: 10.1007/s40262-015-0239-5. PMID: 25647628; PMCID: PMC4513224. 17: Miura Y, Imamura CK, Fukunaga K, Katsuyama Y, Suyama K, Okaneya T, Mushiroda T, Ando Y, Takano T, Tanigawara Y. Sunitinib-induced severe toxicities in a Japanese patient with the ABCG2 421 AA genotype. BMC Cancer. 2014 Dec 16;14:964. doi: 10.1186/1471-2407-14-964. PMID: 25515134; PMCID: PMC4301945. 18: Teo YL, Chue XP, Chau NM, Tan MH, Kanesvaran R, Wee HL, Ho HK, Chan A. Association of drug exposure with toxicity and clinical response in metastatic renal cell carcinoma patients receiving an attenuated dosing regimen of sunitinib. Target Oncol. 2015 Sep;10(3):429-37. doi: 10.1007/s11523-014-0349-2. Epub 2014 Dec 13. PMID: 25502986. 19: Yu H, Steeghs N, Kloth JS, de Wit D, van Hasselt JG, van Erp NP, Beijnen JH, Schellens JH, Mathijssen RH, Huitema AD. Integrated semi-physiological pharmacokinetic model for both sunitinib and its active metabolite SU12662. Br J Clin Pharmacol. 2015 May;79(5):809-19. doi: 10.1111/bcp.12550. PMID: 25393890; PMCID: PMC4415717. 20: Narjoz C, Cessot A, Thomas-Schoemann A, Golmard JL, Huillard O, Boudou- Rouquette P, Behouche A, Taieb F, Durand JP, Dauphin A, Coriat R, Vidal M, Tod M, Alexandre J, Loriot MA, Goldwasser F, Blanchet B. Role of the lean body mass and of pharmacogenetic variants on the pharmacokinetics and pharmacodynamics of sunitinib in cancer patients. Invest New Drugs. 2015 Feb;33(1):257-68. doi: 10.1007/s10637-014-0178-2. Epub 2014 Oct 25. PMID: 25344452.