[CAS NO. 2358775-70-7] PROTACCRBNDegrader-1

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PRODUCTS SPECIFICATIONS [2358775-70-7]

Catalog

AS1132224

Brand

Arctom Scientific

CAS

2358775-70-7

DESCRIPTION [2358775-70-7]

Overview

MDL	-
Molecular Weight	1061.25
Molecular Formula	C53H72N8O13S
SMILES	O=C(NC1=O)CCC1N(C2=O)C(C3=C2C(NCCNC(COCCCCCOCCOCCCCCOCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O)=CC=C3)=O

For research use only. We do not sell to patients.

Summary

PROTAC CRBN Degrader-1 comprises a cereblon ( CRBN ) ligand binding group, a linker and an von Hippel-Landau (VHL) binding group. PROTAC CRBN Degrader-1 is an cereblon (CRBN) degrader ^[1] .

IC50 & Target

VHL

Cereblon

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 94.23 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.9423 mL	4.7114 mL	9.4229 mL
5 mM	0.1885 mL	0.9423 mL	1.8846 mL
10 mM	0.0942 mL	0.4711 mL	0.9423 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 5 mg/mL (4.71 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 5 mg/mL (4.71 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 5 mg/mL (4.71 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Girardini M, et al. Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs. Bioorg Med Chem. 2019 Jun 15;27(12):2466-2479.