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.
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| 名称 | SGC2085 free base |
|---|---|
| Iupac 化学名称 | (S)-2-amino-N-(4-(3,5-dimethylphenoxy)-3-methylbenzyl)propanamide |
| 同义词 | 1821908-49-9 (HCl) 1821908-48-8 (free base) |
| 分子式 | C19H24N2O2 |
| 分子量 | 312.413 |
| Smile | C[C@H](N)C(NCC1=CC=C(OC2=CC(C)=CC(C)=C2)C(C)=C1)=O |
| InChiKey | GLFOFXKMALJTCZ-HNNXBMFYSA-N |
| InChi | InChI=1S/C19H24N2O2/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)/t15-/m0/s1 |
| Cas号 | 1821908-48-8 (free base) |
| Related CAS |
| Packaging | 价格 | Availability | 纯度 | Shipping Time |
|---|---|---|---|---|
| Bulk | 询价 | 询价 | 询价 |
| Formulation | Solid powder |
|---|---|
| 纯度 | 98% Min. |
| 存储 | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| 可溶性 | Soluble in DMSO |
| Handling | |
| 运输条件 | 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. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
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. PubMed PMID: 27390919.