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Merck

100069

17-DMAG

A potent antitumor analog of 17-AAG that binds to the ATPase site of human Hsp90α with high affinity and displays excellent bioavailability and aqueous solubility.

Synonym(s):

17-DMAG, NSC 707545, 17-Desmethoxy-17-N,N-dimethylaminoethylamino-geldanamycin, HCl, 17-N,N-Dimethylaminoethylamino-17-demethoxy-geldanamycin, HCl, 17DMAG

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About This Item

Empirical Formula (Hill Notation):
C32H48N4O8 · xHCl
CAS Number:
467214-21-7
Molecular Weight:
616.75 (free base basis)
MDL number:
MFCD00011291
UNSPSC Code:
12352200
NACRES:
NA.77

Product Name

17-DMAG, A potent antitumor analog of 17-AAG that binds to the ATPase site of human Hsp90α with high affinity and displays excellent bioavailability and aqueous solubility.

InChI

1S/C32H48N4O8.ClH/c1-18-14-22-27(34-12-13-36(5)6)24(37)17-23(29(22)39)35-31(40)19(2)10-9-11-25(42-7)30(44-32(33)41)21(4)16-20(3)28(38)26(15-18)43-8;/h9-11,16-18,20,25-26,28,30,34,38H,12-15H2,1-8H3,(H2,33,41)(H,35,40);1H/b11-9-,19-10+,21-16+;/t18-,20+,25+,26+,28-,30+;/m1./s1

InChI key

DFSYBWLNYPEFJK-IHLRWNDRSA-N

assay

≥95% (TLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

purple

solubility

water: 10 mg/mL
DMSO: 5 mg/mL

shipped in

wet ice

storage temp.

−20°C

Quality Level

100

Related Categories

General description

A cell-permeable, water soluble, potent anti-tumor analog of 17-AAG (Cat. No. 100068) that binds to the ATPase site of human Hsp90α with high affinity (GI50 = 51 nM for 17-DMAG vs. 120 nM for 17-AAG in the NCI 60-cell panel in vitro activity screen).
A potent antitumor analog of 17-AAG (Cat. No. 100068 ) that binds to the ATPase site of human Hsp90α with high affinity (GI50 = 51 nM for 17-DMAG vs. 120 nM for 17-AAG in the NCI 60-cell panel in vitro activity screen), and displays excellent bioavailability and aqueous solubility.

Biochem/physiol Actions

Cell permeable: no
GI50 = 51 nM for 17-DMAG vs. 120 nM for 17-AAG in the NCI 60-cell panel in vitro activity screen
Primary Target
17-DMAG
Product does not compete with ATP.
Reversible: no

Disclaimer

Toxicity: Standard Handling (A)

Other Notes

Tian, Z.Q., et al. 2004. Bioorg. Med. Chem.12, 5317.
Jez, J.M., et al. 2003. Chem. Biol.10, 361.
Egorin, M.J., et al. 2002. Cancer Chemother. Pharmacol.49, 7.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Behnoush Khaledian et al.
Cancer science, 112(3), 1225-1234 (2020-12-29)
We have previously identified receptor tyrosine kinase-like orphan receptor 1 (ROR1) as a direct transcriptional target of TTF-1/NKX2-1, a lineage-survival oncogene in lung adenocarcinoma. ROR1 sustains prosurvival signaling from multiple receptor tyrosine kinases including epidermal growth factor receptor, MET, and

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