Ravoxertinib GMP is Ravoxertinib (HY-15947) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Ravoxertinib (GDC-0994) is an orally active ERK1/2 inhibitor. Ravoxertinib inhibits the ERK1/2 MAPK signaling pathway and reduces the expression levels of c-Myc, HK2 and LDHA. Ravoxertinib decreases mammosphere formation, and exerts additive and/or superadditive cytotoxicity when combined with Ipatasertib (HY-15186) in 3D tumor sphere models. Ravoxertinib can be used in research related to various cancers including breast cancer, melanoma, head and neck cancer, non-small cell lung cancer, ovarian cancer and Merkel cell carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 1453848-26-4
- Formula: C21H18ClFN6O2
- Molecular Weight:440.86
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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ERK1 |
ERK2 |
In relevant in vitro experiments on stem cell-like human glioma stem cells, Ravoxertinib GMP completely abrogates Humanin (HY-P1928)-induced Temozolomide (HY-17364) resistance, restores the growth inhibitory effect of Temozolomide on tumor cells, and inhibits the Humanin-induced upregulation of Hus1 protein expression[1].
Combination of Ravoxertinib GMP (0.1-10 μM; 7 d) and ipatasertib induces additive to superadditive cytotoxicity in multiple human tumor organoid spheres, with over 2-log cell killing achieved in the 417821-307-R-J1 lung squamous cell carcinoma organoid spheres[2].
Ravoxertinib GMP (1 μM; 72 h) does not significantly inhibit the LMCD1-mediated enhancement of cell proliferation in human dermal fibroblasts[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:417821-307-R-J1 lung squamous-cell carcinoma, LG0567-F671 NSCLC, 138582-337-R-J1 Merkel cell tumor, 845751-090-R-J2 HNSCC, 171881-019-R-J1 breast carcinoma, 327498-153-R-J2 uterine sarcoma, 349418-098-R NSCLC, 989133-093-R-J1 NSCLC, MDA-MB-231 breast carcinoma, SK-OV-3 ovarian carcinoma (in multi-cell type 3D tumor spheroids with HUVECs and hMSCs)
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Concentration:0.1-10 μM (in combination with ipatasertib)
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Incubation Time:7 days
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Result:Produced more than 2-logs of cytotoxicity in 417821-307-R-J1 lung squamous-cell carcinoma mct-spheroids.
Resulted in additive cytotoxicity with 1- to 2-logs of cytotoxicity in 9 tested cell lines.
Showed sub-additive to additive effects in LG0567-F671 NSCLC mct-spheroids via surface plot analysis.
Exhibited regions of greater-than-additive cytotoxicity across ipatasertib concentrations in 138582-337-R-J1 Merkel cell tumor, 845751-090-R-J2 HNSCC, and 171881-019-R-J1 breast carcinoma mct-spheroids.
Ravoxertinib GMP (20-30 mg/kg; p.o.) is well tolerated at 20 mg/kg and 30 mg/kg in NSG mice bearing 845751-090-R-J2 head and neck squamous cell carcinoma PDX, but its combination with ipatasertib does not control tumor growth, leading to progressive disease[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-scid gamma mice (NSG) (female, 6 weeks old, ~26 g, breast carcinoma PDX model)[2]
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Dosage:20 mg/kg; 30 mg/kg
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Administration:p.o.
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Result:Was well tolerated at 20 mg/kg and 30 mg/kg.
Resulted in progressive disease when combined with ipatasertib (60 mg/kg) at 30 mg/kg.
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Animal Model:NOD-scid gamma mice (NSG) (female, 6 weeks old, ~26 g, head and neck squamous cell carcinoma PDX model)[2]
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Dosage:20 mg/kg; 30 mg/kg
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Administration:p.o.
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Result:Was well tolerated at 20 mg/kg and 30 mg/kg.
Resulted in progressive disease when combined with ipatasertib (60 mg/kg) at 30 mg/kg.
Chemical Information
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CAS No. 1453848-26-4
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Molecular Weight 440.86
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Formula C21H18ClFN6O2
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SMILES
O=C1C=C(C2=NC(NC3=CC=NN3C)=NC=C2)C=CN1[C@@H](C4=CC=C(Cl)C(F)=C4)CO
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Synonyms
GDC-0994 (GMP)
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[2]. Teicher BA, et al. Targeted therapy combinations with ipatasertib in multi-cell type 3D tumor spheroid models. Acad Oncol. 2025;2(2):10.20935/acadonco7726. [Content Brief]
[3]. Ye Z, et al. LMCD1 facilitates the induction of pluripotency via cell proliferation, metabolism, and epithelial-mesenchymal transition. Cell Biol Int. 2022;46(9):1409-1422. [Content Brief]
[4]. Hunt BG, et al. RON-augmented cholesterol biosynthesis in breast cancer metastatic progression and recurrence. Oncogene. 2023;42(21):1716-1727. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ravoxertinib (GMP) Related Classifications
HY-15947G Related Classifications
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