MI-503
- Product Name
- MI-503
- CAS No.
- 1857417-13-0
- Chemical Name
- MI-503
- Synonyms
- mi503;M1-503;mi-503;CS-1946;MI503;MI 503;Inhibitor,MI503,inhibit,MI 503,MI-503,Epigenetic Reader Domain;1-((1H-Pyrazol-4-yl)methyl)-4-methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-;1-((1H-Pyrazol-4-yl)methyl)-4-methyl-5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile;1H-Indole-2-carbonitrile, 4-methyl-1-(1H-pyrazol-4-ylmethyl)-5-[[4-[[6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl]amino]-1-piperidinyl]methyl]-
- CBNumber
- CB22747932
- Molecular Formula
- C28H27F3N8S
- Formula Weight
- 564.63
- MOL File
- 1857417-13-0.mol
MI-503 Property
- Boiling point:
- 782.9±60.0 °C(Predicted)
- Density
- 1.48±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 50 mg/mL (88.55 mM);Water : < 0.1 mg/mL (insoluble)
- form
- Solid
- pka
- 14.10±0.50(Predicted)
- color
- White to off-white
- InChIKey
- DETOMBLLEOZTMZ-UHFFFAOYSA-N
- SMILES
- N1(CC2=CNN=C2)C2=C(C(C)=C(CN3CCC(NC4N=CN=C5SC(CC(F)(F)F)=CC5=4)CC3)C=C2)C=C1C#N
N-Bromosuccinimide Price
- Product number
- 456198
- Product name
- MI-503
- Packaging
- 1mg
- Price
- $779
- Updated
- 2021/12/16
- Product number
- M350055
- Product name
- MI-503
- Packaging
- 2.5mg
- Price
- $935
- Updated
- 2021/12/16
- Product number
- CS-6217
- Product name
- MI-503
- Purity
- 99.81%
- Packaging
- 2mg
- Price
- $140
- Updated
- 2021/12/16
- Product number
- BM170658
- Product name
- MI 503
- Packaging
- 5mg
- Price
- $220
- Updated
- 2021/12/16
- Product number
- CS-6217
- Product name
- MI-503
- Purity
- 99.81%
- Packaging
- 5mg
- Price
- $240
- Updated
- 2021/12/16
MI-503 Chemical Properties,Usage,Production
Uses
MI-503 is used in the pharmacological inhibition of menin-MLL interaction that blocks progression of MLL leukemia in vivo.
Biochem/physiol Actions
MI-503 is a highly potent menin-MLL interaction inhibitor (cell-free IC50 = 14.7 nM against 1 nM FITC-MLL(4-13) peptide; cellular IC50 = 220 nM using HEK293 MLL-AF9 fusion transfectants) that targets menin MLL-binding site with high affinity (KD = 9.3 nM by ITC). MI-503 selectively inhibits mixed lineage leukemia (MLL) oncogenic fusion-driven cancer progression in cultures (GI50 from 250 to 570 nM; GI50 >5 μM against cells without MLL gene translocation) and is efficacious against human MLL leukemia MV4; tumor growth in mice in vivo (by 80-100%; 60 mg/kg/day i.p.) with good pharmacokinetic properties, oral bioavailability (73% post 30 mg/kg p.o.), and no adverse effects to the animals.
in vitro
MI-503 occupies the F9 and P13 pockets on menin, forming a hydrogen bond with Tyr276, and also extends beyond the P13 pocket to form hydrogen bonds with Trp341 and Glu366. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-503 results in substantial growth inhibition, with GI50 of 0.22 μM. The cell growth inhibitory effect of MI-503 is time-dependent, with a pronounced impact achieved after 7-10 days of treatment.
in vivo
MI-503 achieves a high level in peripheral blood following a single intravenous or oral dose while also showing high oral bioavailability (75%). MI-503 induces strong tumor growth inhibition with once-daily intraperitoneal (i.p.) administration. Treatment with MI-503 results in an over 80% reduction in MV4, 11 tumor volume, and complete tumor regression in two mice. Ten consecutive days of treatment with MI-503 results in a marked delay in the progression of mLL leukemia in mice and significantly reduces leukemia tumor burden. Treatment with MI-503 and MI-463 leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of mLL fusion proteins substantially upregulated in mLL leukemias.
MI-503 Preparation Products And Raw materials
Raw materials
Preparation Products
MI-503 Suppliers
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View Lastest Price from MI-503 manufacturers
- Product
- MI-503 1857417-13-0
- Price
- US $0.00-0.00/mg
- Min. Order
- 1mg
- Purity
- 98%+ HPLC
- Supply Ability
- 50g per month
- Release date
- 2024-03-28