Molecular structure of GW2974, CAS Number: 202272-68-2
GW2974 (CAS 202272-68-2)
Alternate Names:
N4-(1-Benzyl-1H-indazol-5-yl)-N6,N6-dimethyl-pyrido [3,4-d]pyrimidine-4,6-diamine
Application:
GW2974 is a selective dual EGFR and Neu (ErbB-2) inhibitor
CAS Number:
202272-68-2
Purity:
≥98%
Molecular Weight:
395.47
Molecular Formula:
C23H21N7
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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Description
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SDS & Certificate of Analysis
GW2974 is a dual selective inhibitor of EGFR and Neu (ErbB-2) receptor tyrosine kinases. It is known that tyrosine kinases are transmembrane proteins, which are essential in cell growth and survival. Studies indicate that GW2974 inhibits cancer line PC-3 (sc-2220) growth, via its ability to inhibit tyrosine kinases. In addition, GW2974 stimulates the amount of NSE and Chr-A (chromogranin A) in cells. Studies involving BK5.erbB2 mice show that GW2974 inhibits 12-O-tetradecanoylphorbol-13-acetate-induced epidermal hyperproliferation, which resulted in a lower expression of EGFR and Neu. Furthermore, these studies suggest that the inhibitory effects on cell growth of GW2974 is more potent during tumor promotion and when Neu is overexpressed.
GW2974 (CAS 202272-68-2) References
- Effects of the ErbB1/ErbB2 kinase inhibitor GW2974 on androgen-independent prostate cancer PC-3 cell line growth and NSE, chromogranin A and osteopontin content. | Terracciano, D., et al. 2010. Oncol Rep. 24: 213-7. PMID: 20514464
- Dual inhibition of both the epidermal growth factor receptor and erbB2 effectively inhibits the promotion of skin tumors during two-stage carcinogenesis. | Kiguchi, K., et al. 2010. Cancer Prev Res (Phila). 3: 940-52. PMID: 20682802
- GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. | Sodani, K., et al. 2012. Biochem Pharmacol. 83: 1613-22. PMID: 22414725
- Activation of the epidermal growth factor receptor promotes lymphangiogenesis in the skin. | Marino, D., et al. 2013. J Dermatol Sci. 71: 184-94. PMID: 23706492
- EGF receptor-dependent mechanism may be involved in the Tamm-Horsfall glycoprotein-enhanced PMN phagocytosis via activating Rho family and MAPK signaling pathway. | Li, KJ., et al. 2014. Molecules. 19: 1328-43. PMID: 24451252
- Protein-bound uremic toxins induce tissue remodeling by targeting the EGF receptor. | Sun, CY., et al. 2015. J Am Soc Nephrol. 26: 281-90. PMID: 25012179
- Overexpression of microRNA-133b is associated with the increased survival of patients with hepatocellular carcinoma after curative hepatectomy: Involvement of the EGFR/PI3K/Akt/mTOR signaling pathway. | Wang, X., et al. 2017. Oncol Rep. 38: 141-150. PMID: 28586051
- Knockdown of SLC34A2 inhibits cell proliferation, metastasis, and elevates chemosensitivity in glioma. | Bao, Z., et al. 2019. J Cell Biochem. 120: 10205-10214. PMID: 30592329
- Epidermal growth factor receptor controls glycogen phosphorylase in T cells through small GTPases of the RAS family. | Llavero, F., et al. 2019. J Biol Chem. 294: 4345-4358. PMID: 30647127
- A drug-repositioning screen using splicing-sensitive fluorescent reporters identifies novel modulators of VEGF-A splicing with anti-angiogenic properties. | Star, E., et al. 2021. Oncogenesis. 10: 36. PMID: 33941763
- 5-(Indol-2-yl)pyrazolo[3,4-b]pyridines as a New Family of TASK-3 Channel Blockers: A Pharmacophore-Based Regioselective Synthesis. | Ramírez, D., et al. 2021. Molecules. 26: PMID: 34202296
- GW-2974 and SCH-442416 modulators of tyrosine kinase and adenosine receptors can also stabilize human telomeric G-quadruplex DNA. | Salem, AA., et al. 2022. PLoS One. 17: e0277963. PMID: 36476719
- Targeting EGFR/PI3K/AKT/mTOR Signaling in Hepatocellular Carcinoma. | Bang, J., et al. 2023. Pharmaceutics. 15: PMID: 37631344
Inhibitor of:
EGFR, and Neu.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
GW2974, 25 mg | sc-252869 | 25 mg | $240.00 |