1-BOC-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER

Names

[ Name ]:
1-BOC-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER

[Synonym ]:
1-O-tert-butyl 3-O-methyl azetidine-1,3-dicarboxylate
1-BOC-AZETIDINE-3-CARBOXYLICACIDMETHYLESTER

Biological Activity

[Description]:

Methyl 1-Boc-azetidine-3-carboxylate is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Methyl 1-Boc-azetidine-3-carboxylate is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Antibody-drug Conjugate >> ADC Linker

Signaling Pathways >> PROTAC >> PROTAC Linker

[Target]

Non-cleavable

[In Vitro]

ADCs are comprised of an antibody to which is attached an ADC cytotoxin through an ADC linker[1]. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[2].

[References]

[1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.

[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
269.0±33.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₀H₁₇NO₄

[ Molecular Weight ]:
215.246

[ Flash Point ]:
116.5±25.4 °C

[ Exact Mass ]:
215.115753

[ PSA ]:
55.84000

[ LogP ]:
0.73

[ Vapour Pressure ]:
0.0±0.6 mmHg at 25°C

[ Index of Refraction ]:
1.481

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Hazard Codes ]:
Xi

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%