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CX-6258 hydrochloride hydrate
CX-6258 hydrochloride hydrate
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CAS No.:
1353858-99-7
Price valid (until):
2026-08-18
Company Type:
Manufactory
Location:
United States
Qualification:
Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName CX-6258 hydrochloride hydrate Cat No CEI-1298 Product Overview IC50 Value: 5 nM (Pim 1); 25 nM (Pim 2); 16 nM (Pim 3). CX-6258 is a potent, orally efficacious pan-Pim kinases Inhibitor with excellent biochemical potency and kinase selectivity. in vitro: CX-6258 inhibited Flt-3 and Pim-3 (IC50=0.134 and 0.016 uM). At 0.5 uM of CX-6258, only Pim-1, Pim-2, Pim-3, and Flt-3 of the 107 kinases tested were inhibited by more than 80%, showing excellent selectivity. CX-6258 was also shown to be a reversible inhibitor of Pim-1 (Ki=0.005 uM). CX-6258 showed robust antiproliferative potencies against all cell lines tested derived from human solid tumors and hematological malignancies. In mechanistic cellular assays with MV-4-11 human AML cells, caused dose-dependent inhibition of the phosphorylation of 2 pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. Pim-1 inhibition using the small molecule inhibitor CX-6258 (12 mM, 3 h) diminishes endogenous NKX3.1 steady state levels in 22RV1 and LNCaP cells. CX-6258 treatment (12 mM, 3 h) treatment diminished steady-state levels of ectopic NKX3.1 in PC3 cells. CX-6258 treatment resulted in a significant reduction in NKX3.1 half-life. While ectopically expressed NKX3.1 in control cells had a half-life of _90 min, Pim-1 inhibition reduced the half-life to _52 min. in vivo: CX-6258 showed dose-dependent efficacy in mice bearing MV-4-11 xenografts, with 45% and 75% TGI at 50 and 100 mg/kg/day, respectively. Treatment of mice bearing PC3 xenografts with CX-6258 p. o. 50 mg/kg was also well tolerated and produced 51% TGI. CAS No 1353858-99-7 Molecular Weight 516.42 Storage Store at -20°C Synonyms CX6258 hydrochloride hydrate; CX 6258 hydrochloride hydrate Targets Pan-Pim kinases Molecular Formula C26H27Cl2N3O4 Solubility 25°C: DMSO Shipping Conditions Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request category Specialty Chemicals(c26) cas_num 1353858-99-7 Basic Info-
Product Name:
CX-6258 (hydrochloride hydrate)
CAS No.:1353858-99-7
Categories:
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Seller Information
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Business Type:
Manufactory
-
Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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