商品编号


6327



品牌


Tocris



公司


Bio-Techne Corporation



公司分类


Ligases



Size

5 mg

商品信息

Description:
(+)-JQ1 based PROTAC that selectively degrades BRD4 in cells

Chemical Name:
(6
S
)-4-(4-Chlorophenyl)-
N
-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1
H
-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6
H
-thieno[3,2-
f
][1,2,4]triazolo[4,3-
a
][1,4]diazepine-6-acetamide

Purity:
≥98% (HPLC)


BIOLOG
ical Activity Technical Data Solubility Calculators Datasheets References


BIOLOG
ical Activity

PROTAC comprising BET antago
NIST
(+)-JQ1 (Cat.No. 4499) conjugated to a cereblon E3 ubiquitin ligase ligand. Depletes BRD4 in cancer cell lines
in vitro
(EC
50
= 430 nM in breast cancer cells) and induces apoptosis. Delays tumor growth and downregulates MYC in mice bearing human AML xenografts.



Licensing Information

Sold under license from Dana-Farber Cancer Institute.



Technical Data



M. Wt

785.27



Formula

C
38
H
37
ClN
8
O
7
S



Storage

Store at -20°C



Purity

≥98% (HPLC)



CAS Number

1799711-21-9



PubChem ID

91799313



InChI Key

LKEGXJXRNBALBV-PMCHYTPCSA-N



Smiles

CC1=NN=C2[C@@H](N=C(C3=CC=C(C=C3)Cl)C4=C(N12)SC(C)=C4C)CC(NCCCCNC(COC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)=O



The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All
Tocris
products are intended for laboratory research use only.



Solubility Data




Solvent

Max Conc. mg/mL

Max Conc. mM



Solubility



DMSO

78.53

100





Preparing Stock Solutions

The following data is based on the
product
molecular weight
785.27
. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.



Concentration / Solvent Volume / Mass

1 mg

5 mg

10 mg



1 mM

1.27 mL

6.37 mL

12.73 mL



5 mM

0.25 mL

1.27 mL

2.55 mL



10 mM

0.13 mL

0.64 mL

1.27 mL



50 mM

0.03 mL

0.13 mL

0.25 mL






Molarity Calculator






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Reconstitution Calculator






Reconstitution Calculator



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Product Datasheets


Certificate of Analysis / Product Datasheet


Safety Datasheet

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References

References are publications that support the products'
BIOLOG
ical activity.


Winter

et al
(2015) Drug Development. Phthalimide conjugation as a strategy for
in vivo
target protein degradation. Science
348
1376 PMID: 25999370


Wurz

et al
(2017) A "
Click chemistry
platform" for the rapid synthesis of bispecific molecules for inducing protein degradation. J.Med.Chem. 10.1021 PMID: 28378579




Keywords: dBET1, supplier, Proteolysis, Targeting, Chimera, PROTAC, cereblon, E3, ubiquitin, ligase, bromodomain, BRD4, degradation, Ubiquitin, E3, Ligases,
Tocris
Bioscience