MI-463
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $750 | To Be Confirmed |
| 250mg | $1450 | To Be Confirmed |
| 1g | $2175 | To Be Confirmed |
: Cat #: V2601 CAS #: 1628317-18-9 Purity ≥ 98%
Description: MI-463 is a novel potent & orally bioactive inhibitor of Menin-MLL interaction with an IC50 value of 15.3 nM.
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| Molecular Weight (MW) | 484.54 |
|---|---|
| Molecular Formula | C24H23F3N6S |
| CAS No. | 1628317-18-9 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 96 mg/mL (198.1 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 22 mg/mL (45.4 mM) | |
| SMILES Code | CC1=C2C(NC(C#N)=C2)=CC=C1CN(CC3)CCC3NC4=C(C=C(CC(F)(F)F)S5)C5=NC=N4 |
| Synonyms | MI-463; MI 463; MI463. |
| Protocol | In Vitro | MI-463 can reach the target protein in mammalian cells and effectively inhibit the menin-mLL-AF9 interaction at sub-micromolar concentrations. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-463 results in substantial growth inhibition, with GI50 of 0.23 μM. |
|---|---|---|
| In Vivo | MI-463 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (45%). Pharmacologic inhibition of the menin-mLL interaction substantially delays progression of mLL leukemia in murine models through on-target activity without causing toxicity. MI-463 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. The expression of mLL fusion protein target genes, HOXA9 and MEIS1, are significant reduced upon treatment with MI-463. 20 days treatment of MV4;11 xenograft recipient mice with MI-463 also results in a substantial delay in leukemia progression as manifested by a marked decrease in the bioluminescence level which is associated with a significant decrease in the population of leukemic cells in the peripheral blood, spleen and bone marrow samples. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0638 mL | 10.3191 mL | 20.6381 mL | 41.2763 mL |
| 5mM | 0.4128 mL | 2.0638 mL | 4.1276 mL | 8.2553 mL |
| 10mM | 0.2064 mL | 1.0319 mL | 2.0638 mL | 4.1276 mL |
| 20mM | 0.1032 mL | 0.5160 mL | 1.0319 mL | 2.0638 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.