Free shipping on all orders over $ 500

MI-503

Cat. No. M9151
MI-503 Structure
Size Price Availability Quantity
5mg USD 255  USD255 In stock
10mg USD 440  USD440 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

MI-503 is a potent and selective Menin-MLL inhibitor with IC50 of 14.7 nM. MI-503 shows pronounced growth suppressive activity in a panel of human MLL leukemia cell lines(GI50 at 250 nM-570 nM range), but only a minimal effect in human leukemia cell lines without MLL translocations. MI-503 is also very effective in inducing differentiation of MLL leukemia cells and substantially increases expression of CD11b, a myeloid differentiation marker. These effects are accompanied by reduced c-kit (CD117) expression, a marker associated with leukemia stem cells (LSCs).

In vivo, MI-503 blocks hematologic tumors in vivo and reduces MLL leukemia tumor burden. MI-503 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (~75%). Prolonged treatment (38 days) with MI-503 induces no toxicity in mice as reflected by no alterations in the body weight and no morphological changes in liver and kidney tissues.

Chemical Information
Molecular Weight 564.63
Formula C28H27F3N8S
CAS Number 1857417-13-0
Solubility (25°C) DMSO: ≥ 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ichiroh Kato, et al. Menin‑MLL inhibitors induce ferroptosis and enhance the anti‑proliferative activity of auranofin in several types of cancer cells

[2] Laurie K Svoboda, et al. Menin regulates the serine biosynthetic pathway in Ewing sarcoma

[3] Katarzyna Kempinska, et al. Pharmacologic Inhibition of the Menin-MLL Interaction Leads to Transcriptional Repression of PEG10 and Blocks Hepatocellular Carcinoma

[4] Laurie K Svoboda, et al. Tumorigenicity of Ewing sarcoma is critically dependent on the trithorax proteins MLL1 and menin

[5] Dmitry Borkin, et al. Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo

Related Histone Methyltransferase Products
SAH-EZH2

SAH-EZH2, a stable EZH2 α-helical peptide, is an EZH2/EED interaction inhibitor.

UNC4976

UNC4976 is a positive allosteric modulator (PAM) peptidomimetic of CBX7 chromodomain binding to nucleic acids.

C21

C21 is a potent, irreversible, and selective PRMT1 inhibitor with an IC50 of 1.8 μM.

EZH2-IN-15

EZH2-IN-15 (SHR2554) is a EZH2 inhibitor.

NSD-IN-2

NSD-IN-2 is a potent and irreversible NSD1 inhibitor.

  Catalog
Abmole Inhibitor Catalog




Keywords: MI-503 supplier, Histone Methyltransferase, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.