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CX-6258 hydrochloride hydrate
CAS No. 1353858-99-7
CX-6258 hydrochloride hydrate( CX6258 hydrochloride hydrate )
Catalog No. M11441 CAS No. 1353858-99-7
A potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 100MG | Get Quote | In Stock |
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| 200MG | 897 | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameCX-6258 hydrochloride hydrate
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NoteResearch use only, not for human use.
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Brief DescriptionA potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively.
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DescriptionA potent, selective, and orally efficacious pan-Pim inhibitor with IC50 of 5/25/16 nM for Pim1/2/3, respectively; exhibits in vitro synergy with chemotherapeutics and robust in vivo efficacy in driven tumor models; also decreases steady state levels and half-life of NKX3.1 protein but not mRNA in prostate cancer cells.Blood Cancer Discontinued.
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In VitroCX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells.CX-6258 treatment results in a significant reduction in NKX3.1 half-life.Western Blot Analysis Cell Line:MV-4-11 human AML cells.Concentration:0.1 μM, 1 μM, 10 μM.Incubation Time:2 hours.Result:Caused dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.
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In VivoCX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models. Animal Model:Nude mice, MV-4-11 xenograft models Dosage:50 mg/kg, 100 mg/kg.Administration:Oral administration; once daily; over a period of 21 days.Result:Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.
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SynonymsCX6258 hydrochloride hydrate
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PathwayJAK/STAT Signaling
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TargetPim
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RecptorPim
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Research AreaCancer
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IndicationBlood cancer
Chemical Information
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CAS Number1353858-99-7
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Formula Weight516.4163
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Molecular FormulaC26H27Cl2N3O4
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Purity>98% (HPLC)
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Solubility10 mM in DMSO
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SMILESCN1CCCN(CC1)C(=O)C2=CC=CC(=C2)C3=CC=C(O3)C=C4C5=C(C=CC(=C5)Cl)NC4=O.O.Cl
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Chemical Name2H-Indol-2-one, 5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-, hydrochloride, hydrate (1:1:1), (3E)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Haddach M, et al. ACS Med Chem Lett. 2011 Dec 27;3(2):135-9.
2. Padmanabhan A, et al. J Cell Biochem. 2013 May;114(5):1050-7.
3. Rebello RJ, et al. Clin Cancer Res. 2016 Nov 15;22(22):5539-5552.
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