GEN-1 | RORγt inverse agonist

MedKoo Cat#: 128190 | Name: GEN-1

Description:

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

GEN-1 is a RORγt inverse agonist.

Chemical Structure

GEN-1

CAS#N/A

Theoretical Analysis

MedKoo Cat#: 128190

Name: GEN-1

CAS#: N/A

Chemical Formula: C24H31N3O3S

Exact Mass: 441.2086

Molecular Weight: 441.59

Elemental Analysis: C, 65.28; H, 7.08; N, 9.52; O, 10.87; S, 7.26

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

GEN-1; GEN1; GEN 1

IUPAC/Chemical Name

N-(4-(4-acetylpiperazin-1-yl)benzyl)-N-cyclobutyl-1-phenylmethanesulfonamide

InChi Key

KIHDXHLXSMPQSN-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H31N3O3S/c1-20(28)25-14-16-26(17-15-25)23-12-10-21(11-13-23)18-27(24-8-5-9-24)31(29,30)19-22-6-3-2-4-7-22/h2-4,6-7,10-13,24H,5,8-9,14-19H2,1H3

SMILES Code

O=C(C)N1CCN(C2=CC=C(CN(C3CCC3)S(=O)(CC4=CC=CC=C4)=O)C=C2)CC1

Appearance

To be determined

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 441.59 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: Thaker PH, Borys N, Fewell J, Anwer K. GEN-1 immunotherapy for the treatment of ovarian cancer. Future Oncol. 2019 Feb;15(4):421-438. doi: 10.2217/fon-2018-0423. Epub 2018 Oct 16. PMID: 30325199. 2: Thaker PH, Bradley WH, Leath CA 3rd, Gunderson Jackson C, Borys N, Anwer K, Musso L, Matsuzaki J, Bshara W, Odunsi K, Alvarez RD. GEN-1 in Combination with Neoadjuvant Chemotherapy for Patients with Advanced Epithelial Ovarian Cancer: A Phase I Dose-escalation Study. Clin Cancer Res. 2021 Oct 15;27(20):5536-5545. doi: 10.1158/1078-0432.CCR-21-0360. Epub 2021 Jul 29. PMID: 34326131; PMCID: PMC9338778. 3: Starosta W, Leciejewicz J. Bis[[(6-carb-oxy-pyridazine-3-carboxyl-ato- κN,O)lithium]-μ-penta-hydrogen-dioxy-gen(1+)]. Acta Crystallogr Sect E Struct Rep Online. 2010 Oct 9;66(Pt 11):m1362-3. doi: 10.1107/S1600536810039176. PMID: 21588805; PMCID: PMC3009182. 4: Lozinšek M. Nitro-sonium tetra-fluorido-borate, NOBF₄. IUCrdata. 2021 Nov 18;6(Pt 11):x211215. doi: 10.1107/S2414314621012153. PMID: 36337464; PMCID: PMC9462292. 5: Yin X, Davi R, Lamont EB, Thaker PH, Bradley WH, Leath CA 3rd, Moore KM, Anwer K, Musso L, Borys N. Historic Clinical Trial External Control Arm Provides Actionable GEN-1 Efficacy Estimate Before a Randomized Trial. JCO Clin Cancer Inform. 2023 Jan;7:e2200103. doi: 10.1200/CCI.22.00103. PMID: 36608308. 6: Spatola BN, Lo JY, Wang B, Curran SP. Nuclear and cytoplasmic WDR-23 isoforms mediate differential effects on GEN-1 and SKN-1 substrates. Sci Rep. 2019 Aug 13;9(1):11783. doi: 10.1038/s41598-019-48286-y. PMID: 31409866; PMCID: PMC6692315. 7: Thaker PH, Brady WE, Lankes HA, Odunsi K, Bradley WH, Moore KN, Muller CY, Anwer K, Schilder RJ, Alvarez RD, Fracasso PM. A phase I trial of intraperitoneal GEN-1, an IL-12 plasmid formulated with PEG-PEI-cholesterol lipopolymer, administered with pegylated liposomal doxorubicin in patients with recurrent or persistent epithelial ovarian, fallopian tube or primary peritoneal cancers: An NRG Oncology/Gynecologic Oncology Group study. Gynecol Oncol. 2017 Nov;147(2):283-290. doi: 10.1016/j.ygyno.2017.08.001. Epub 2017 Aug 10. PMID: 28802766; PMCID: PMC5704992. 8: Chen M. Correlation between ORange (Gen 1, pseudophakic) intraoperative refraction and 1-week postcataract surgery autorefraction. Clin Ophthalmol. 2011;5:197-9. doi: 10.2147/OPTH.S17489. Epub 2011 Feb 11. PMID: 21383949; PMCID: PMC3045070. 9: Medina E, Rueda C, Batlle D. FSGS and COVID-19 in Non-African American Patients. Kidney360. 2023 May 1;4(5):687-699. doi: 10.34067/KID.0000000000000104. PMID: 37229730; PMCID: PMC10371264. 10: Zang Y, Thall PF, Yuan Y. A generalized phase 1-2-3 design integrating dose optimization with confirmatory treatment comparison. Biometrics. 2024 Jan 29;80(1):ujad022. doi: 10.1093/biomtc/ujad022. PMID: 38364811; PMCID: PMC10873567.