| Identification | More | [Name]
XMD8-92 | [CAS]
1234480-50-2 | [Synonyms]
XMD 8-92
XMD 8-92 (free base)
2-((2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl)amino)-5,11-dimethyl-5H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6(11H)-one
2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one
2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one XMD 8-92
XMD 8-92 2-[[2-Ethoxy-4-(4-hydroxy-1-piperidinyl)phenyl]amino]-5,11-dihydro-5,11-dimethyl-6H-pyrimido[4,5-b][1,4]benzodiazepin-6-one | [Molecular Formula]
C26H30N6O3 | [MDL Number]
MFCD18782742 | [MOL File]
1234480-50-2.mol | [Molecular Weight]
475 |
| Chemical Properties | Back Directory | [Boiling point ]
741.8±70.0 °C(Predicted) | [density ]
1.301 | [storage temp. ]
Store at 4°C | [solubility ]
≥23.75 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
solid | [pka]
14.76±0.20(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
XMD8-92 is an ERK5 inhibitor (Kd = 80 nM) that less potently inhibits DCAMKL2, TNK1, and Plk4 (Kds = 190, 890, and 600 nM, respectively) in a panel of 402 kinases.1 It blocks ERK5 autophosphorylation, ERK5-mediated phosphorylation of promyelocytic leukemia protein (PML), and PML-dependent activation of p21.1 XMD8-92 inhibits AP-1 transcriptional activity induced by MEK5-activated ERK5 but not that induced by Cdc37.2 It inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice and reduces tumor growth in a HeLa mouse xenograft model when administered at a dose of 50 mg/kg twice per day.1 XMD8-92 also binds bromodomain-containing protein 4 (BRD4; Kd = 170 nM for BRD4 bromodomain 1).3 | [Uses]
XMD 8-92, is a BMK1 inhibitor and a highly selective inhibitor of ERK5 activity. XMD8-92 blocks cellular BMK1 activation and significantly suppresses tumor growth in lung and cervical tumor models and is well tolerated in animals. | [Definition]
ChEBI: XMD8-92 is a dimethylpyrimido[4,5-b][1,4]benzodiazepin-6-one carrying at C-2 on the pyrimidine ring a [2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl]amino substituent. It is an inhibitor of the BMK1 kinase pathway. It has a role as a protein kinase inhibitor. | [in vivo]
XMD8-92 (i.p.; twice a day for 28 days) significantly inhibits the growth of the xenografted human tumors[1]. | Animal Model: | HeLa Xenograft Model (6-week-old Nod/Scid mice)[1] | | Dosage: | 50 mg/kg | | Administration: | I.p.; twice a day for 28 days | | Result: | Significantly inhibited the growth of the xenografted human tumors.
|
| [IC 50]
BMK1: 80 nM (Kd); BRD4: 190 nM (Kd) | [storage]
Store at 4°C |
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| Company Name: |
Moltt Biocem Co., Ltd.
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+86-21-38682181 15900741819 |
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www.approvedhomemanagement.com/ShowSupplierProductsList15856/0.htm |
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