GW2974
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    WARNING: This product is for research use only, not for human or veterinary use.

Hodoodo CAT#: H341193

CAS#: 202272-68-2

Description: GW2974 Potent and selective dual inhibitor of EGFR.

Chemical Structure

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GW2974
CAS# 202272-68-2
Instruction

Theoretical Analysis

Hodoodo Cat#: H341193
Name: GW2974
CAS#: 202272-68-2
Chemical Formula: C23H21N7
Exact Mass: 395.19
Molecular Weight: 395.470
Elemental Analysis: C, 69.85; H, 5.35; N, 24.79

Price and Availability

Size Price Availability Quantity
50mg USD 550 2 Weeks
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Synonym: GW2974; GW-2974; GW 2974.

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

InChi Key: DYYZXRCFCVDSKD-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: CN(C)C1=CC2=C(NC3=CC4=C(N(CC5=CC=CC=C5)N=C4)C=C3)N=CN=C2C=N1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 395.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

11: Agarwal S, Zerillo C, Kolmakova J, Christensen JG, Harris LN, Rimm DL, Digiovanna MP, Stern DF. Association of constitutively activated hepatocyte growth factor receptor (Met) with resistance to a dual EGFR/Her2 inhibitor in non-small-cell lung cancer cells. Br J Cancer. 2009 Mar 24;100(6):941-9. doi: 10.1038/sj.bjc.6604937. Epub 2009 Feb 24. PubMed PMID: 19240716; PubMed Central PMCID: PMC2661782.

12: Shell SA, Lyass L, Trusk PB, Pry KJ, Wappel RL, Bacus SS. Activation of AMPK is necessary for killing cancer cells and sparing cardiac cells. Cell Cycle. 2008 Jun 15;7(12):1769-75. Epub 2008 Jun 30. PubMed PMID: 18594201.

13: Lu J, Rho O, Wilker E, Beltran L, Digiovanni J. Activation of epidermal akt by diverse mouse skin tumor promoters. Mol Cancer Res. 2007 Dec;5(12):1342-52. doi: 10.1158/1541-7786.MCR-07-0115. PubMed PMID: 18171992.

14: Li P, Ge HB, Sun Z. [Inhibiting effects of GW2974 on DMBA-induced hamster buccal pouch carcinogenesis]. Zhonghua Kou Qiang Yi Xue Za Zhi. 2007 Jul;42(7):432-5. Chinese. PubMed PMID: 17961367.

15: Sun Z, Sood S, Li N, Yang P, Newman RA, Yang CS, Chen X. Chemoprevention of 7,12-dimethylbenz[a]anthracene (DMBA)-induced oral carcinogenesis in hamster cheek pouch by topical application of a dual inhibitor of epidermal growth factor receptor (EGFR) and ErbB2 tyrosine kinases. Oral Oncol. 2008 Jul;44(7):652-7. Epub 2007 Oct 23. PubMed PMID: 17936675; PubMed Central PMCID: PMC2546572.

16: Spector NL, Yarden Y, Smith B, Lyass L, Trusk P, Pry K, Hill JE, Xia W, Seger R, Bacus SS. Activation of AMP-activated protein kinase by human EGF receptor 2/EGF receptor tyrosine kinase inhibitor protects cardiac cells. Proc Natl Acad Sci U S A. 2007 Jun 19;104(25):10607-12. Epub 2007 Jun 7. PubMed PMID: 17556544; PubMed Central PMCID: PMC1965560.

17: Witters LM, Witkoski A, Planas-Silva MD, Berger M, Viallet J, Lipton A. Synergistic inhibition of breast cancer cell lines with a dual inhibitor of EGFR-HER-2/neu and a Bcl-2 inhibitor. Oncol Rep. 2007 Feb;17(2):465-9. PubMed PMID: 17203189.

18: Coley HM, Shotton CF, Ajose-Adeogun A, Modjtahedi H, Thomas H. Receptor tyrosine kinase (RTK) inhibition is effective in chemosensitising EGFR-expressing drug resistant human ovarian cancer cell lines when used in combination with cytotoxic agents. Biochem Pharmacol. 2006 Oct 16;72(8):941-8. Epub 2006 Aug 24. PubMed PMID: 16934227.

19: Kiguchi K, Ruffino L, Kawamoto T, Ajiki T, Digiovanni J. Chemopreventive and therapeutic efficacy of orally active tyrosine kinase inhibitors in a transgenic mouse model of gallbladder carcinoma. Clin Cancer Res. 2005 Aug 1;11(15):5572-80. PubMed PMID: 16061875.