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202272-68-2
  • names:

    N4-(1-Benzyl-1H-indazol-5-yl)-N6,N6-dimethyl-pyrido [3,4-d]pyrimidine-4,6-diamine

  • CAS号:

    202272-68-2

    MDL Number:
  • MF(分子式): C23H21N7 MW(分子量): 395.47
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
GW2974
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中文别名 GW2974
英文别名 GW2974; GW-2974; GW 2974.
CAS号 202272-68-2
SMILES CN(C)C1=CC2=C(NC3=CC4=C(N(CC5=CC=CC=C5)N=C4)C=C3)N=CN=C2C=N1
Inchi InChI=1S/C23H21N7/c1-29(2)22-11-19-20(13-24-22)25-15-26-23(19)28-18-8-9-21-17(10-18)12-27-30(21)14-16-6-4-3-5-7-16/h3-13,15H,14H2,1-2H3,(H,25,26,28)
InchiKey DYYZXRCFCVDSKD-UHFFFAOYSA-N
分子式 Formula C23H21N7
分子量 Molecular Weight 395.47
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 GW2974(CAS:202272-68-2):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionGW2974 Potent and selective dual inhibitor of EGFR.
Application1
Application2
Application3
警示图
危险性 Warning
危险性警示
安全声明
安全防护
备注
[1]Wang X, Zeng J, Wang L, Zhang X, Liu Z, Zhang H, Dong J. 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. Oncol Rep. 2017 Jul;38(1):141-150. doi: 10.3892/or.2017.5699. Epub 2017 Jun 6. PubMed PMID: 28586051.
[2]Chakraborty AK, Mehra R, Digiovanna MP. Co-targeting ER and HER family receptors induces apoptosis in HER2-normal or overexpressing breast cancer models. Anticancer Res. 2015 Mar;35(3):1243-50. PubMed PMID: 25750271.
[3] Li KJ, Siao SC, Wu CH, Shen CY, Wu TH, Tsai CY, Hsieh SC, Yu CL. EGF receptor-dependent mechanism may be involved in the Tamm-Horsfall glycoprotein-enhanced PMN phagocytosis via activating Rho family and MAPK signaling pathway. Molecules. 2014 Jan 21;19(1):1328-43. doi: 10.3390/molecules19011328. PubMed PMID: 24451252.
[4] Wang L, Liu Q, Zhao H, Cui K, Yao L, Nie F, Jin G, Hao A, Wong ST. Differential effects of low- and high-dose GW2974, a dual epidermal growth factor receptor and HER2 kinase inhibitor, on glioblastoma multiforme invasion. J Neurosci Res. 2013 Jan;91(1):128-37. doi: 10.1002/jnr.23140. Epub 2012 Nov 1. PubMed PMID: 23115024.
[5] Sodani K, Tiwari AK, Singh S, Patel A, Xiao ZJ, Chen JJ, Sun YL, Talele TT, Chen ZS. GW583340 and GW2974, human EGFR and HER-2 inhibitors, reverse ABCG2- and ABCB1-mediated drug resistance. Biochem Pharmacol. 2012 Jun 15;83(12):1613-22. doi: 10.1016/j.bcp.2012.02.028. Epub 2012 Mar 7. PubMed PMID: 22414725; PubMed Central PMCID: PMC3360928.
6: Xia W, Liu Z, Zong R, Liu L, Zhao S, Bacus SS, Mao Y, He J, Wulfkuhle JD, Petricoin EF 3rd, Osada T, Yang XY, Hartman ZC, Clay TM, Blackwell KL, Lyerly HK, Spector NL. Truncated ErbB2 expressed in tumor cell nuclei contributes to acquired therapeutic resistance to ErbB2 kinase inhibitors. Mol Cancer Ther. 2011 Aug;10(8):1367-74. doi: 10.1158/1535-7163.MCT-10-0991. Epub 2011 Jun 14. PubMed PMID: 21673090; PubMed Central PMCID: PMC3836594.7: Rajabalian S, Hajializadeh Z, Pooraboli I, Jangi-Aghdam H, Badinloo M. Establishment, characterization, and drug sensitivity of a new Ewing sarcoma cell line (SS-ES-1). J Pediatr Hematol Oncol. 2010 Nov;32(8):e331-7. doi: 10.1097/MPH.0b013e3181ee4d16. Erratum in: J Pediatr Hematol Oncol. 2011 Apr;33(3):247. Badinloo, Marziyeh [added]. PubMed PMID: 20962673.8: Kiguchi K, Kitamura T, Moore T, Rumi M, Chang HC, Treece D, Ruffino L, Connolly K, DiGiovanni J. Dual inhibition of both the epidermal growth factor receptor and erbB2 effectively inhibits the promotion of skin tumors during two-stage carcinogenesis. Cancer Prev Res (Phila). 2010 Aug;3(8):940-52. doi: 10.1158/1940-6207.CAPR-10-0010. Epub 2010 Aug 3. PubMed PMID: 20682802; PubMed Central PMCID: PMC2940063.9: Terracciano D, Mazzarella C, Di Carlo A, Mariano A, Ferro M, Di Lorenzo G, Giordano A, Altieri V, De Placido S, Macchia V. 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. Oncol Rep. 2010 Jul;24(1):213-7. PubMed PMID: 20514464.10: Wonders KY, Hydock DS, Greufe S, Schneider CM, Hayward R. Endurance exercise training preserves cardiac function in rats receiving doxorubicin and the HER-2 inhibitor GW2974. Cancer Chemother Pharmacol. 2009 Nov;64(6):1105-13. doi: 10.1007/s00280-009-0967-z. Epub 2009 Apr 8. PubMed PMID: 19352663.1
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