| Identification | Back Directory | [Name]
MU 380 | [CAS]
2109805-78-7 | [Synonyms]
MU 380
Pyrazolo[1,5-a]pyrimidin-7-amine, 6-bromo-5-(3R)-3-piperidinyl-3-[1-(trifluoromethyl)-1H-pyrazol-4-yl]- | [Molecular Formula]
C15H15BrF3N7 | [MOL File]
2109805-78-7.mol | [Molecular Weight]
430.23 |
| Chemical Properties | Back Directory | [density ]
1.92±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
8.86±0.10(Predicted) | [color ]
white to beige | [SMILES]
NC1=C(C([C@@]2([H])CNCCC2)=NC3=C(C=NN13)C4=CN(N=C4)C(F)(F)F)Br |
| Hazard Information | Back Directory | [Uses]
MU380 is a potent and selective CHK1 inhibitor that induces apoptosis and has anticancer activity[1]. | [Biological Activity]
MU380 is a metabolically stable analog of CHK1 inhibitor SCH900776 (MK8776) does not undergo in vivo N-dealkylation. MU380 is a potent and selective CHK1 inhibitorwhich potently sensitizes multiple cancer cell lines to DNA antimetabolites including hydroxyureacytarabine and gemcitabine. | [in vivo]
MU380 (20 mg/kg, in 20% aqueous Kolliphor solution, every three days from day 14 to day 28) can effectively inhibit tumor growth in NOD-scid?IL2Rγnull?mice with tumour[1].
| Animal Model: | NOD-scid?IL2Rγnull?mice[1] | | Dosage: | 20 mg/kg | | Administration: | In 20% aqueous Kolliphor solution, every three days from day 14 to day 28 | | Result: | Significantly inhibit the growth of tumors and gradually reduce their volume, with an average reduction of about 61%. |
| [References]
[1] Miroslav Boudny, et al. Novel CHK1 inhibitor MU380 exhibits significant single-agent activity in TP53-mutated chronic lymphocytic leukemia cells. Haematologica. 2019 Dec;104(12):2443-2455. DOI:10.3324/haematol.2018.203430 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|