GDC-0994 (Synonyms: Ravoxertinib) |
Catalog No.GC12006
One-Click Copy Product Info
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GDC-0994 (GDC-0994) es un inhibidor de la cinasa ERK activo por vÍa oral con una IC50 de 6,1 nM y 3,1 nM para ERK1 y ERK2, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1453848-26-4
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
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Cell lines |
BRAFV600E cell lines |
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Preparation method |
The solubility of this compound in DMSO is >22.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Applications |
In BRAFV600E cell lines, treatment with GDC-0994 resulted in stronger pathway inhibition and subsequent suppression of cell proliferation when compared to BRAF inhibitors. |
| Animal experiment [2]: | |
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Animal models |
Mice bearing KRAS-mutant and BRAF-mutant human xenograft tumors, HT29 colorectal cancer xenograft model. |
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Dosage form |
Oral administration, daily |
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Application |
Daily, oral administration of GDC-0994 resulted in significant single-agent activity in KRAS-mutant and BRAF-mutant human xenograft tumors in mice. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Nambu T, Iwai K, Shibata S, et al. Identification of driver of anti-tumor activity of TAK-931 in human colorectal cancer xenograft model[J]. European Journal of Cancer, 2016, 69: S30. [2]. 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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| Cas No. | 1453848-26-4 | SDF | |
| Sinónimos | Ravoxertinib | ||
| Chemical Name | (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 | ||
| Canonical SMILES | CN1C(NC2=NC=CC(C(C=CN3[C@](C4=CC(F)=C(Cl)C=C4)([H])CO)=CC3=O)=N2)=CC=N1 | ||
| Formula | C21H18ClFN6O2 | M.Wt | 440.86 |
| Solubility | ≥ 44.1mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2683 mL | 11.3415 mL | 22.6829 mL |
| 5 mM | 453.7 μL | 2.2683 mL | 4.5366 mL |
| 10 mM | 226.8 μL | 1.1341 mL | 2.2683 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)