GDC-0994ERK1/2 inhibitor CAS# 1453848-26-4 |
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Quality Control & MSDS
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| Cas No. | 1453848-26-4 | SDF | Download SDF |
| PubChem ID | 71727581 | Appearance | Powder |
| Formula | C21H18ClFN6O2 | M.Wt | 440.86 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Ravoxertinib | ||
| Solubility | DMSO : ≥ 35 mg/mL (79.39 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 1-[(1S)-1-(4-chloro-3-fluorophenyl)-2-hydroxyethyl]-4-[2-[(2-methylpyrazol-3-yl)amino]pyrimidin-4-yl]pyridin-2-one | ||
| SMILES | CN1C(=CC=N1)NC2=NC=CC(=N2)C3=CC(=O)N(C=C3)C(CO)C4=CC(=C(C=C4)Cl)F | ||
| Standard InChIKey | RZUOCXOYPYGSKL-GOSISDBHSA-N | ||
| Standard 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | GDC-0994 is an orally bioavailable inhibitor selective for ERK kinase activity with IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.In Vitro:GDC-0994 also inhibits p90RSK with IC50 of 12 nM[1]. GDC-0994 is highly selective for ERK1 and ERK2, with biochemical potency of 1.1 nM and 0.3 nM, respectively[2].In Vivo:In CD-1 mice, a 10 mg/kg oral dose of GDC-0994 is sufficient to achieve the desired target coverage for at least 8 h[1]. 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[2]. References: | |||||
GDC-0994 Dilution Calculator
GDC-0994 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2683 mL | 11.3415 mL | 22.6829 mL | 45.3659 mL | 56.7073 mL |
| 5 mM | 0.4537 mL | 2.2683 mL | 4.5366 mL | 9.0732 mL | 11.3415 mL |
| 10 mM | 0.2268 mL | 1.1341 mL | 2.2683 mL | 4.5366 mL | 5.6707 mL |
| 50 mM | 0.0454 mL | 0.2268 mL | 0.4537 mL | 0.9073 mL | 1.1341 mL |
| 100 mM | 0.0227 mL | 0.1134 mL | 0.2268 mL | 0.4537 mL | 0.5671 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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GDC-0994 is a potent and selective inhibitor of ERK1/2 with IC50 values of 1.1 and 0.3 nM, respectively [1].
The extracellular-signal-regulated kinases (ERK1 and ERK2) are members of the MAP kinase family and act downstream of the RAS/RAF/MEK/ERK signaling cascade that are commonly activated by upstream oncogenic signaling or oncogenic mutations in BRAF or RAS. ERK1/2 play important roles in proliferation, differentiation and cell cycle progression [1].
GDC-0994 is an orally available and potent ERK1/2 inhibitor with potential antineoplastic activity. In mice bearing KRAS-mutant and BRAF-mutant human xenograft tumors, GDC-0994 exhibited significant single-agent activity and inhibited phospho-p90RSK [1]. When orally administration, GDC-0994 inhibited both activation of ERK-mediated signal transduction pathways and ERK phosphorylation, which then inhibited ERK-dependent tumor cell survival and proliferation.
References:
[1]. Robarge K, Schwarz J, Blake J, et al. Abstract DDT02-03: Discovery of GDC-0994, a potent and selective ERK1/2 inhibitor in early clinical development. AACR Annual Meeting, 2014, San Diego, CA.
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Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-y l)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.[Pubmed:27227380]
J Med Chem. 2016 Jun 23;59(12):5650-60.
The extracellular signal-regulated kinases ERK1/2 represent an essential node within the RAS/RAF/MEK/ERK signaling cascade that is commonly activated by oncogenic mutations in BRAF or RAS or by upstream oncogenic signaling. While targeting upstream nodes with RAF and MEK inhibitors has proven effective clinically, resistance frequently develops through reactivation of the pathway. Simultaneous targeting of multiple nodes in the pathway, such as MEK and ERK, offers the prospect of enhanced efficacy as well as reduced potential for acquired resistance. Described herein is the discovery and characterization of GDC-0994 (22), an orally bioavailable small molecule inhibitor selective for ERK kinase activity.
