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主营:抗癌化学试剂和激酶抑制剂
℡ 4000-520-616
℡ 4000-520-616
MedKoo/GDC-0879featured/5mg/401470
产品编号:401470
市  场 价:¥5900.00
场      地:美国(厂家直采)
产品分类: 蛋白类>多肽>多肽合成>
联系QQ:1570468124
电话号码:4000-520-616
邮      箱: info@ebiomall.com
美  元  价:$295.00
品      牌: MedKoo
公      司:MedKoo Biosciences, Inc
公司分类:
MedKoo/GDC-0879featured/5mg/401470
商品介绍

GDC-0879
featured

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

MedKoo CAT#:401470

CAS#:905281-76-7

Description:GDC-0879 is a highly selective, potent, and orally bioavailable RAF small-molecule inhibitor. In GDC-0879 -treated mice, both cell line- and patient-derived BRAF(V600E) tumors exhibited stronger and more sustained pharmacodynamic inhibition (>90% for 8 hours) and improved survival compared with mutant KRAS-expressing tumors.

Price and Availability

SizePriceShipping out timeQuantity
5mgUSD 2952 Weeks
10mgUSD 4502 Weeks
25mgUSD 8952 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-01-23.Prices are subject to change without notice.

GDC-0879, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 401470Name: GDC-0879CAS#: 905281-76-7Chemical Formula: C19H18N4O2Exact Mass: 334.14298Molecular Weight: 334.37182Elemental Analysis:C, 68.25; H, 5.43; N, 16.76; O, 9.57

Synonym:GDC0879; GDC-0879; GDC 0879.

IUPAC/Chemical Name:(E)-5-(1-(2-hydroxyethyl)-3-(pyridin-4-yl)-1H-pyrazol-4-yl)-2,3-dihydro-1H-inden-1-one oxime

InChi Key:DEZZLWQELQORIU-RELWKKBWSA-N

InChi Code:InChI=1S/C19H18N4O2/c24-10-9-23-12-17(19(21-23)13-5-7-20-8-6-13)15-1-3-16-14(11-15)2-4-18(16)22-25/h1,3,5-8,11-12,24-25H,2,4,9-10H2/b22-18+

SMILES Code:OCCN1N=C(C2=CC=NC=C2)C(C3=CC4=C(/C(CC4)=N/O)C=C3)=C1

Technical Data

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, not in water

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

Additional Information

 GDC-0879 is a highly selective, novel potent, orally bioavailable B-Raf inhibitor in various in vitro and cell-based assays with an IC50 estimate of 0.13 nM against purified B-Raf V600E enzyme and a cellular pERK IC50 of 63 nM in the MALME-3M cell line GDC-0879 is a highly selective, novel potent, orally bioavailable B-Raf inhibitor in various in vitro and cell-based assays with an IC50 estimate of 0.13 nM against purified B-Raf V600E enzyme and a cellular pERK IC50 of 63 nM in the MALME-3M cell line

References

1: Mooz J, Oberoi-Khanuja TK, Harms GS, Wang W,Jaiswal BS, Seshagiri S, Tikkanen R, Rajalingam K. Dimerization of thekinase ARAF promotes MAPK pathway activation and cell migration. SciSignal. 2014 Aug 5;7(337):ra73. doi: 10.1126/scisignal.2005484. PubMedPMID: 25097033.

2: Doma E, Rupp C, Varga A, Kern F, Riegler B, Baccarini M. Skintumorigenesis stimulated by Raf inhibitors relies upon Raf functionsthat are dependent and independent of ERK. Cancer Res. 2013 Dec1;73(23):6926-37. doi: 10.1158/0008-5472.CAN-13-0748. Epub 2013 Oct 15.PubMed PMID: 24129679.

3: Coffee EM, Faber AC, Roper J, Sinnamon MJ, Goel G, Keung L, Wang WV,Vecchione L, de Vriendt V, Weinstein BJ, Bronson RT, Tejpar S, XavierRJ, Engelman JA, Martin ES, Hung KE. Concomitant BRAF and PI3K/mTORblockade is required for effective treatment of BRAF(V600E) colorectalcancer. Clin Cancer Res. 2013 May 15;19(10):2688-98. doi:10.1158/1078-0432.CCR-12-2556. Epub 2013 Apr 2. Erratum in: Clin CancerRes. 2013 Jul 15;19(14):4018. PubMed PMID: 23549875; PubMed CentralPMCID: PMC3815598.

4: Fuchs O. Targeting of NF-kappaB signaling pathway, other signalingpathways and epigenetics in therapy of multiple myeloma. CardiovascHematol Disord Drug Targets. 2013 Mar 1;13(1):16-34. Review. PubMedPMID: 23534949.

5: Chou B, Adler RS, Meng M, Percey S, Dean B, Hop CE, Shin YG.Validation and application of a liquid chromatography-tandem massspectrometric method for the determination of GDC-0879 and itsmetabolite in dog plasma using solid phase extraction. J Pharm BiomedAnal. 2012 Nov;70:354-61. doi: 10.1016/j.jpba.2012.05.029. Epub 2012 Jun1. PubMed PMID: 22717139.

6: Hu J, Yu H, Kornev AP, Zhao J, Filbert EL, Taylor SS, Shaw AS.Mutation that blocks ATP binding creates a pseudokinase stabilizing thescaffolding function of kinase suppressor of Ras, CRAF and BRAF. ProcNatl Acad Sci U S A. 2011 Apr 12;108(15):6067-72. doi:10.1073/pnas.1102554108. Epub 2011 Mar 25. PubMed PMID: 21441104; PubMedCentral PMCID: PMC3076888.

7: Hatzivassiliou G, Song K, Yen I, Brandhuber BJ, Anderson DJ, AlvaradoR, Ludlam MJ, Stokoe D, Gloor SL, Vigers G, Morales T, Aliagas I, Liu B,Sideris S, Hoeflich KP, Jaiswal BS, Seshagiri S, Koeppen H, Belvin M,Friedman LS, Malek S. RAF inhibitors prime wild-type RAF to activate theMAPK pathway and enhance growth. Nature. 2010 Mar 18;464(7287):431-5.doi: 10.1038/nature08833. Epub 2010 Feb 3. PubMed PMID: 20130576.

8: Choo EF, Driscoll JP, Feng J, Liederer B, Plise E, Randolph N, ShinY, Wong S, Ran Y. Disposition of GDC-0879, a B-RAF kinase inhibitor inpreclinical species. Xenobiotica. 2009 Sep;39(9):700-9. doi:10.1080/00498250902991827. PubMed PMID: 19552528.

9: Hoeflich KP, Herter S, Tien J, Wong L, Berry L, Chan J, O"Brien C,Modrusan Z, Seshagiri S, Lackner M, Stern H, Choo E, Murray L, FriedmanLS, Belvin M. Antitumor efficacy of the novel RAF inhibitor GDC-0879 ispredicted by BRAFV600E mutational status and sustained extracellularsignal-regulated kinase/mitogen-activated protein kinase pathwaysuppression. Cancer Res. 2009 Apr 1;69(7):3042-51. doi:10.1158/0008-5472.CAN-08-3563. Epub 2009 Mar 10. PubMed PMID: 19276360.

10: Wong H, Belvin M, Herter S, Hoeflich KP, Murray LJ, Wong L, Choo EF.Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinaseinhibitor: understanding relationships between systemic concentrations,phosphorylated mitogen-activated protein kinase kinase 1 inhibition, andefficacy. J Pharmacol Exp Ther. 2009 Apr;329(1):360-7. doi:10.1124/jpet.108.148189. Epub 2009 Jan 15. PubMed PMID: 19147858.

品牌介绍
MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(Research Triangle Park, 简称 RTP ),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中    文美帝药库医药科技公司创立于2008年总部位于美国东海岸
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