GMB 475

BCR-ABL1 kinase PROTAC® Degrader. Induces degradation of BCR-ABL1 and cABL1, inhibits downstream STAT5 signaling and suppresses cell proliferation in chronic myeloid leukemia cells lines.

Product information

CAS Number: 2490599-18-1

Molecular Weight: 861.93

Formula: C43H46F3N7O7S

Synonym:

GMB475

GMB-475

Chemical Name: (2S)-1-((R)-3,3-dimethyl-2-(2-(2-(4-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)phenoxy)ethoxy)acetamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

Smiles: CC(C)(C)[C@H](NC(=O)COCCOC1=CC=C(C=C1)C1=CC(NC2=CC=C(C=C2)OC(F)(F)F)=NC=N1)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC1=CC=C(C=C1)C1SC=NC=1C

InChiKey: ONDVWISBMHHLGZ-SBJIGXGQSA-N

InChi: InChI=1S/C43H46F3N7O7S/c1-26-38(61-25-50-26)29-7-5-27(6-8-29)21-47-40(56)35-19-31(54)22-53(35)41(57)39(42(2,3)4)52-37(55)23-58-17-18-59-32-13-9-28(10-14-32)34-20-36(49-24-48-34)51-30-11-15-33(16-12-30)60-43(44,45)46/h5-16,20,24-25,31,35,39,54H,17-19,21-23H2,1-4H3,(H,47,56)(H,52,55)(H,48,49,51)/t31-,35+,39-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (290.05 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

References:

1. Burslem GM, Schultz AR, Bondeson DP, Eide CA, Savage Stevens SL, Druker BJ, Crews CM. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation. Cancer Res. 2019 Sep 15;79(18):4744-4753.

Products are for research use only. Not for human use.