1. GLL398

GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models.

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GLL398 Chemical Structure

GLL398 Chemical Structure

CAS No. : 2077980-80-2

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Description

GLL398, an orally active selective estrogen receptor degrader (SERD), competitively binds to the estrogen receptor with an IC50 value of 1.14 nM. GLL398 exhibits a strong dose-dependent binding profile for the ER with a Y537S point mutation (IC50= 29.5 nM). GLL398 blocks tumor growth in xenograft breast cancer models[1].

In Vitro

GLL398 is a boron-modified GW5638 analog[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

398.26

Formula

C25H23BO4

CAS No.
SMILES

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

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (627.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5109 mL 12.5546 mL 25.1092 mL
5 mM 0.5022 mL 2.5109 mL 5.0218 mL
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Purity & Documentation

Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5109 mL 12.5546 mL 25.1092 mL 62.7731 mL
5 mM 0.5022 mL 2.5109 mL 5.0218 mL 12.5546 mL
10 mM 0.2511 mL 1.2555 mL 2.5109 mL 6.2773 mL
15 mM 0.1674 mL 0.8370 mL 1.6739 mL 4.1849 mL
20 mM 0.1255 mL 0.6277 mL 1.2555 mL 3.1387 mL
25 mM 0.1004 mL 0.5022 mL 1.0044 mL 2.5109 mL
30 mM 0.0837 mL 0.4185 mL 0.8370 mL 2.0924 mL
40 mM 0.0628 mL 0.3139 mL 0.6277 mL 1.5693 mL
50 mM 0.0502 mL 0.2511 mL 0.5022 mL 1.2555 mL
60 mM 0.0418 mL 0.2092 mL 0.4185 mL 1.0462 mL
80 mM 0.0314 mL 0.1569 mL 0.3139 mL 0.7847 mL
100 mM 0.0251 mL 0.1255 mL 0.2511 mL 0.6277 mL
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
GLL398
Cat. No.:
HY-101119
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