MT-802

• Description:

  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].

• 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  Cereblon

• CAS Number:

  [2231744-29-7]