| Identification | Back Directory | [Name]
UNC-2371A | [CAS]
1429882-07-4 | [Synonyms]
UNC2371
MRX-2843
UNC-2371A
UNC2371;MRX-2843
MRX-2843 (UNC2371)
MRX-2843?(Synonyms: UNC2371
(1r,4r)-4-(2-(2-cyclopropylethylamino)-5-(4-((4-methylpiperazin-1-yl)methyl)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclohexanol
Cyclohexanol, 4-[2-[(2-cyclopropylethyl)amino]-5-[4-[(4-methyl-1-piperazinyl)methyl]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-, trans- | [Molecular Formula]
C29H40N6O | [MDL Number]
MFCD28502224 | [MOL File]
1429882-07-4.mol | [Molecular Weight]
488.67 |
| Chemical Properties | Back Directory | [Melting point ]
>137°C (dec.) | [Boiling point ]
697.3±65.0 °C(Predicted) | [density ]
1.31±0.1 g/cm3(Predicted) | [storage temp. ]
Refrigerator | [solubility ]
Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly, Heated, Sonicated) | [form ]
Solid | [pka]
14.63±0.40(Predicted) | [color ]
White to Pale Beige |
| Hazard Information | Back Directory | [Description]
MRX-2843 is an inhibitor of Mer and FMS-like tyrosine kinase 3 (FLT3; IC50s = 1.3 and 1 nM, respectively). It also inhibits Axl and Tyro3 (IC50s = 15 and 17 nM, respectively). MRX-2843 (10-300 nM) inhibits Mer phosphorylation in MOLM-14 and MV4-11 acute myeloid leukemia (AML) cells and reduces clonal expansion of Kasumi-1 AML cells (IC50 = 143.5 nM). In vivo, MRX-2843 increases survival in NOMO-1 and MOLM-14 AML mouse xenograft models when administered at doses of 65 and 50 mg/kg, respectively. | [Uses]
MRX-2843, is an orally available small-molecule inhibitor of both MERTK and FLT3. | [in vivo]
MRX-2843 is 78% orally bioavailable at a dose of 3 mg/kg with a Cmax of 1.3 μM and a t1/2 of 4.4 hours. In MOLM-14 parental xenografts, both quizartinib and MRX-2843 increase median survival compare with that of vehicle-treated mice (172.5 days versus 40 days and 121 days versus 36 days, respectively, P<0.001). In this model, quizartinib is more effective than MRX-2843 (P<0.005), although higher doses of MRX-2843 are not evaluated. In MOLM-14:D835Y xenografts, quizartinib prolongs survival compare with that of vehicle-treated mice, but the effect is minimal (median survival 45 days vs. 36 days, P<0.001). In MOLM-14:F691L xenografts, treatment with MRX-2843 prolongs survival by almost 2-fold in NSG and NSGS mice (median survival 87 vs. 44.5 days and 87 vs. 48 days, respectively, P<0.005). Increased survival is observed in response to treatment with MRX-2843 versus quizartinib, but the difference is only significant in NSG mice[1]. | [References]
[1] WEIHE ZHANG. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor[J]. Journal of Medicinal Chemistry, 2014, 57 16: 7031-7041. DOI: 10.1021/jm500749d
[2] KATHERINE A MINSON. The MERTK/FLT3 inhibitor MRX-2843 overcomes resistance-conferring FLT3 mutations in acute myeloid leukemia.[J]. JCI insight, 2016, 1 3: e85630. DOI: 10.1172/jci.insight.85630 |
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| Company Name: |
ChemCell Biomedicine Co.,Ltd.
|
| Tel: |
020-13556033878 2965585218 13556033878 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15061/0_EN.htm |
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