MT-802

MT-802 is a BTK PROTAC degrader. MT-802 degrades wild-type BTK (DC50 = 14.6 nM) and BTK mutants including E41K, C481S (DC50 = 14.9 nM), C481R, C481Y, C481T, C481F, L528W, and inhibits their Y223 phosphorylation. BI-4732 can be used for the study of Ibrutinib (HY-10997) -resistant chronic lymphocytic leukemia (CLL) . (Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-141371), E3 ligase ligand-linker conjugate (HY-176340) ) [1][2].

Product Specifications

CAS Number

[2231744-29-7]

UNSPSC

12352005

Hazard Statement

H301, H311, H331

Target

Btk; PROTACs

Type

Reference compound

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/mt-802.html

Purity

98.35

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC2=C(C(N(C(CC3)C(NC3=O)=O)C2=O)=O)C=C1)COCCOCCN4CCC(N5N=C(C6=CC=C(OC7=CC=CC=C7)C=C6)C8=C(N)N=CN=C85)CC4

Molecular Formula

C41H41N9O8

Molecular Weight

787.82

Precautions

H301, H311, H331

References & Citations

[1]Lim YS, et al. Orally bioavailable BTK PROTAC active against wild-type and C481 mutant BTKs in human lymphoma CDX mouse models. Blood Adv. 2023 Jan 10;7 (1) :92-105.|[2]Buhimschi AD, et al. Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation. Biochemistry. 2018 Jul 3;57 (26) :3564-3575.