Tanespimycin-d5
Tanespimycin-d5 (17-AAG-d5; NSC 330507-d5; CP 127374-d5) is the deuterium labeled Tanespimycin (HY-10211). Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
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- 화학식: C31H38D5N3O8
- 분자량:590.72
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
제품 설명
In Vitro
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
신청
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled CAS 75747-14-7
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분자량 590.72
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화학식 C31H38D5N3O8
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SMILES
O=C(C(NC(/C(C)=C/C=C\[C@H](OC)[C@H](/C(C)=C/[C@@H]([C@H]([C@H](C[C@@H](C1)C)OC)O)C)OC(N)=O)=O)=CC2=O)C1=C2NC([2H])([2H])/C([2H])=C([2H])/[2H]
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Synonyms
17-AAG-d5; NSC 330507-d5; CP 127374-d5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Kamal A, et al. A high-affinity conformation of Hsp90 confers tumour selectivity on Hsp90 inhibitors. Nature. 2003 Sep 25;425(6956):407-10. [Content Brief]
[2]. Enomoto A, et al. The HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin modulates radiosensitivity by downregulating serine/threonine kinase 38 via Sp1 inhibition. Eur J Cancer. 2013 Nov;49(16):3547-58. [Content Brief]
[3]. Solit DB, et al. 17-Allylamino-17-demethoxygeldanamycin induces the degradation of androgen receptor and HER-2/neu and inhibits the growth of prostate cancer xenografts.Clin Cancer Res, 2002, 8(5), 986-993. [Content Brief]
[4]. Raja, Srikumar M., et al. 17-AAG induces enhanced ubiquitinylation and lysosomal pathway-dependent ErbB2 degradation and cytotoxicity in ErbB2-overexpressing breast cancer cells. Cancer Biology & Therapy (2008), 7(10), 163 [Content Brief]
[5]. Zhang J, et al. The heat shock protein 90 inhibitor 17-AAG suppresses growth and induces apoptosis in human cholangiocarcinoma cells.Clin Exp Med. 2012 Sep 7. [Content Brief]
[6]. Newman B, et al. HSP90 Inhibitor 17-AAG Selectively Eradicates Lymphoma Stem Cells.Cancer Res. 2012 Sep 1;72(17):4551-61. Epub 2012 Jun 29. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)