VTP50469

VTP50469 is a potent, highly selective and orally active inhibitor of Menin-MLL interaction with Ki of 104 pM. VTP50469 exhibits anti-leukemia activity.

Product information

CAS Number: 2169916-18-9

Molecular Weight: 630.82

Formula: C32H47FN6O4S

Chemical Name: 5-Fluoro-N,N-diisopropyl-2-((4-(7-(((1r,4r)-4-(methylsulfonamido)cyclohexyl)methyl)-2,7-diazaspiro[3.5]nonan-2-yl)pyrimidin-5-yl)oxy)benzamide

Smiles: CS(=O)(=O)N[C@@H]1CC[C@@H](CN2CCC3(CN(C3)C3=NC=NC=C3OC3=CC=C(F)C=C3C(=O)N(C(C)C)C(C)C)CC2)CC1

InChiKey: ADHHOUXZPBYYSU-YOCNBXQISA-N

InChi: InChI=1S/C32H47FN6O4S/c1-22(2)39(23(3)4)31(40)27-16-25(33)8-11-28(27)43-29-17-34-21-35-30(29)38-19-32(20-38)12-14-37(15-13-32)18-24-6-9-26(10-7-24)36-44(5,41)42/h8,11,16-17,21-24,26,36H,6-7,9-10,12-15,18-20H2,1-5H3/t24-,26-

Technical Data

Appearance: Solid Power

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

Solubility: DMSO 100 mg/mL (158.52 mM) Ethanol 100 mg/mL (158.52 mM)

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

How to use

In Vitro:

Cell lines carrying MLL-rearrangements are selectively responsive to VTP50469. VTP50469 displaces Menin from protein complexes and inhibits chromatin occupancy of MLL at select genes. Loss of MLL binding leads to changes in gene expression, differentiation, and apoptosis.

In Vivo:

Patient-derived xenograft (PDX) models derived from patients with either MLL-r AML or MLL-r ALL shows dramatic reductions of leukemia burden when treated with VTP50469. Multiple mice engrafted with MLL-r ALL remains disease free greater than one year after treatment.

References:

1. Andrei V. Krivtsov, et al. Cancer Res 2018;78(13 Suppl):Abstract nr 4958.
2. Andrei V Krivtsov, et al. Cancer Cell. 2019 Dec 9;36(6):660-673.

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