Cart
sales@molnova.com
MI-3454
CAS No. 2134169-43-8
MI-3454( —— )
Catalog No. M35130 CAS No. 2134169-43-8
MI-3454 is an orally active, selective and potent inhibitor of Menin-MLL1 interaction that inhibits the proliferation and induces differentiation of acute leukemia cells with MLL1 translocation or NPM1 mutation.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 2MG | 301 | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
-
Product NameMI-3454
-
NoteResearch use only, not for human use.
-
Brief DescriptionMI-3454 is an orally active, selective and potent inhibitor of Menin-MLL1 interaction that inhibits the proliferation and induces differentiation of acute leukemia cells with MLL1 translocation or NPM1 mutation.
-
DescriptionMI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis.
-
In VitroCell Proliferation Assay Cell Line:Murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1 Concentration:0.001, 0.01, 0.1, 1, 10 μM Incubation Time:7 days Result:Demonstrated strong reduction of cell proliferation.RT-PCR Cell Line:Human leukemic cell lines MV-4-11 cells or MOLM13 Concentration:50 nM Incubation Time:6 days Result:Led to downregulated expression of HOXA9 and MEIS1 and expression level of other MLL fusion target genes, including MEF2C, DLX2, HOXA10, PBX3, and FLT3.
-
In VivoAnimal Model:8- to 10-week-old female NSG mice (MV-4-11 xenotransplantation model of MLL leukemia) Dosage:120 mg/kg Administration:Orally; one or twice daily for 7 consecutive daysResult:A once-daily treatment was sufficient to block leukemia progression. Animal Model:Female CD-1 mice Dosage:100 mg/kg (PO) or 15 mg/kg (IV) (Pharmacokinetic Analysis) Administration:PO or IV Result:Had a T1/2 of 3.2 hours, a Cmax of 4698 mg/mL for PO. Had a T1/2 of 2.4 hours, a CL of 2375 mL/hours?kg, and a Vss of 5358 mL/kg for IV.
-
Synonyms——
-
PathwayOthers
-
TargetOther Targets
-
RecptorHistone Methyltransferase
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number2134169-43-8
-
Formula Weight636.73
-
Molecular FormulaC32H35F3N8OS
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 31.25 mg/mL (49.08 mM; Ultrasonic )
-
SMILESCNc1nc(NC2CCN(Cc3ccc4n(CC56CC(C5)(C6)NC=O)c(cc4c3C)C#N)CC2)c2cc(CC(F)(F)F)sc2n1
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
1. Szymon Klossowski, et al. Menin Inhibitor MI-3454 Induces Remission in MLL1-rearranged and NPM1-mutated Models of Leukemia. J Clin Invest. 2020 Feb 3;130(2):981-997.?
molnova catalog
related products
-
Anhydrosafflor yello...
Anhydrosafflor yellow B, isolated from Carthamus tinctorius, inhibits ADP-induced platelet aggregation, exhibits significant anti-oxidative effects in vitro, and possesses certain activity against H2O2-induced cytotoxicity.
-
7-Hydroxy-3-(4-hydro...
7-Hydroxy-3-(4'-hydroxybenzylidene)-chroman-4-one may have anti-inflammatory activity.
-
26-Dimethylaniline
26-Xylidine is an aniline derivative with the chemical formula (CH3)2C6H3NH2. It is an isomer of 24-xylidine and 34-xylidine. It is a colourless liquid although commercial samples can appear to be yellow or even red.
