MedKoo Cat#: 406787 | Name: SGC2085 HCl
Featured

Description:

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

SGC2085 is a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor with an IC50 of 50 nM and more than undred-fold selectivity over other PRMTs. CARM1 is an important positive modulator of Wnt/β-catenin transcription and neoplastic transformation in colorectal cancer as well as a critical factor in estrogen-stimulated breast cancer growth, and its depletion results in decreased proliferation of myeloid leukemia cells in vivo.

Chemical Structure

SGC2085 HCl
CAS#1821908-49-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 406787

Name: SGC2085 HCl

CAS#: 1821908-49-9 (HCl)

Chemical Formula: C19H25ClN2O2

Exact Mass: 0.0000

Molecular Weight: 348.87

Elemental Analysis: C, 65.41; H, 7.22; Cl, 10.16; N, 8.03; O, 9.17

Price and Availability

Size Price Availability Quantity
25mg USD 250.00 2 Weeks
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,750.00 2 Weeks
1g USD 4,250.00 2 Weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
Synonym
SGC2085; SGC-2085; SGC 2085. SGC2085 HCl
IUPAC/Chemical Name
(S)-2-amino-N-(4-(3,5-dimethylphenoxy)-3-methylbenzyl)propanamide hydrochloride
InChi Key
OQGSBQJSJRLNQH-RSAXXLAASA-N
InChi Code
InChI=1S/C19H24N2O2.ClH/c1-12-7-13(2)9-17(8-12)23-18-6-5-16(10-14(18)3)11-21-19(22)15(4)20;/h5-10,15H,11,20H2,1-4H3,(H,21,22);1H/t15-;/m0./s1
SMILES Code
C[C@H](N)C(NCC1=CC=C(OC2=CC(C)=CC(C)=C2)C(C)=C1)=O.[H]Cl
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
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
Related CAS# 1821908-49-9 (SGC2085 hydrochloride); 1821908-48-8 (SGC2085 free base).
Product Data
Biological target:
SGC2085 is a potent and selective inhibitor of CARM1 with an IC50 of 50 nM. SGC2085 also selectively inhibits PRMT6 with an IC50 value of 5.2 μM, but not other PRMT proteins.
In vitro activity:
Two structure-based rounds of optimization produced SGC2085, a CARM1 inhibitor with an IC50 of 50 nM and more than hundred-fold selectivity over other PRMTs. Reference: J Med Chem. 2016 Jul 28;59(14):6838-47. https://pubmed.ncbi.nlm.nih.gov/27390919/
In vivo activity:
To be determined

Preparing Stock Solutions

The following data is based on the product molecular weight 348.87 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
Formulation protocol:
1. Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening. J Med Chem. 2016 Jul 28;59(14):6838-47. doi: 10.1021/acs.jmedchem.6b00668. Epub 2016 Jul 8. Erratum in: J Med Chem. 2016 Aug 25;59(16):7698. PMID: 27390919.
In vitro protocol:
1. Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening. J Med Chem. 2016 Jul 28;59(14):6838-47. doi: 10.1021/acs.jmedchem.6b00668. Epub 2016 Jul 8. Erratum in: J Med Chem. 2016 Aug 25;59(16):7698. PMID: 27390919.
In vivo protocol:
To be determined
Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening. J Med Chem. 2016 Jul 28;59(14):6838-47. doi: 10.1021/acs.jmedchem.6b00668. Epub 2016 Jul 8. Erratum in: J Med Chem. 2016 Aug 25;59(16):7698. doi: 10.1021/acs.jmedchem.6b01095. PMID: 27390919.