Bulk Inquiry
GDC-0994
- Ravoxertinib - RG7842
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C21H18ClFN6O2
- MW: 440.86
Description
GDC-0994 is an orally available small molecule inhibitor of extracellular signal-regulated kinase 1/2 (ERK1/2), highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively. Daily, oral dosing of GDC-0994 results in significant single-agent activity in multiple in vivo cancer models, including KRAS-mutant and BRAF-mutant human xenograft tumors in mice. PD biomarker inhibition of phospho-p90RSK in these tumors correlates with potency in vitro and in vivo. In contrast to other published ERK inhibitors, GDC-0994 neither increases nor decreases phospho-ERK, suggesting that different ERK inhibitors have alternative mechanisms of action with respect to feedback signaling. Furthermore, we demonstrate a novel approach for targeting the oncogenic signaling through the RAS pathway by combining ERK and MEK inhibitors.
More Information
| Parent CAS No. | 1453848-26-4 |
|---|---|
| Chemical Name | (S)-1-(1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-(1-methyl-1H-pyrazol-5-ylamino)pyrimidin-4-yl)pyridin-2(1H)-one |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1(NC2N(C)N=CC=2)N=C(C2C=CN([C@@](CO)([H])C3C=C(F)C(Cl)=CC=3)C(=O)C=2)C=CN=1 |&1:14,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C21H18ClFN6O2/c1-28-19(5-8-25-28)27-21-24-7-4-17(26-21)13-6-9-29(20(31)11-13)18(12-30)14-2-3-15(22)16(23)10-14/h2-11,18,30H,12H2,1H3,(H,24,26,27)/t18-/m1/s1 |
| InChiKey | RZUOCXOYPYGSKL-GOSISDBHSA-N |
| CID | 71727581 |
| Short Description | ERK1/2 inhibitor |
References
- K Robarge et al. Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development.Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA.
- JF Blake et al. Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development J. Med. Chem. 2016, 59(12), 5650-60.
Related Products
| AXON ID | NAME | FROM PRICE |
|---|---|---|
| 1621 | XMD 8-92 trifluoroacetate |
From $77.00 |
| 1694 | FR 180204 |
From $104.50 |
| 1808 | BIX02188-Me |
From $121.00 |
| 1809 | BIX 02189 |
From $121.00 |
| 1846 | XMD 8-92 |
From $77.00 |
| 3197 | Mitochonic acid 5 |
From $99.00 |
| 3803 | SCH900353 |
From Inquiry |
| 3836 | VX-11e |
From Inquiry |
| 3867 | SCH772984 hydrochloride |
From Inquiry |
| 3893 | LY-3214996 |
From Inquiry |
| 4151 | Ulixertinib hydrochloride |
From Inquiry |
| 4284 | EI-52 |
From $154.00 |
Other Categories
Are you sure you would like to remove this item from the shopping cart?
This item is a part of the approved quote. Removing it will remove all quote items from the cart.