GLL398


Catalog No. size PriceQuantity
M7024-2 2mg solid $127
M7024-10 10mg solid $532

Description

Cas:2077980-83-5

Product Information

GLL398 is an Oral Selective Estrogen Receptor Downregulator. GLL398 strongly binds to ERα in a fluorescence resonance energy transfer binding assay (IC50 =1.14 nM) and potently degrades ERα in MCF-7 breast cancer cells (IC50 = 0.21 μM). Most importantly, the introduction of the boronic acid group confers superior oral bioavailability of GLL398 (AUC = 36.9 μg·h/mL) in rats as compared to GW7604 (AUC = 3.35 μg·h/mL). The strikingly favorable pharmacokinetic property of GLL398 makes it a promising oral SERD suitable for clinical evaluation.

 

Chemical Formula: C25H23BO4

 

Exact Mass: 398.1689

 

Molecular Weight: 398.265

 

Elemental Analysis: C, 75.40; H, 5.82; B, 2.71; O, 16.07

 

Synonym: 

 

GLL398

GLL-398

GLL 398

 

Chemical Name:

3-(4-(1-(4-boronophenyl)-2-phenylbut-1-en-1-yl)phenyl)acrylic acid

 

InChi Key: 

BINZFDGAOTWQNC-VZBZSUMNSA-N

 

InChi Code: InChI=1S/C25H23BO4/c1-2-23(19-6-4-3-5-7-19)25(21-13-15-22(16-14-21)26(29)30)20-11-8-18(9-12-20)10-17-24(27)28/h3-17,29-30H,2H2,1H3,(H,27,28)/b17-10+,25-23-

 

Smiles Code:

O=C(O)/C=C/C1=CC=C(/C(C2=CC=C(B(O)O)C=C2)=C(C3=CC=CC=C3)\CC)C=C1

 

 

Technical Data:

 

Appearance: White to off-white solid powder

Purity: >98% (contains E and Z isomers).

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

 

 

References

 

  1. Liu J, Zheng S, Guo S, Zhang C, Zhong Q, Zhang Q, Ma P, Skripnikova EV, Bratton MR, Wiese TE, Wang G. Rational Design of a Boron-Modified Triphenylethylene (GLL398) as an Oral Selective Estrogen Receptor Downregulator. ACS Med Chem Lett. 2016 Nov 29;8(1):102-106. doi: 10.1021/acsmedchemlett.6b00410. eCollection 2017 Jan 12. PubMed PMID: 28105283; PubMed Central PMCID: PMC5238461.

 

Products are for research use only. Not for human use.

Payment & Security

American Express Apple Pay Diners Club Discover Elo Google Pay JCB Mastercard PayPal Shop Pay Venmo Visa

Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.

Estimate shipping

You may also like

Recently viewed