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KW-2478

SKU: orb1223043

Description

KW-2478 is a non-ansamycin HSP90 inhibitor with IC50 of 3.8 nM.(In Vitro):KW-2478 is an inhibitor of Hsp90, with an IC50 of 3.8 nM for Hsp90α. KW-2478 shows anti-proliferative activity against multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI50s of 0.30 μM (OPM-2/GFP), 0.34 μM (KMS-11), 0.39 μM (RPMI 8226), 0.12 μM (NCI-H929), 0.36 μM (Raji), 0.098 μM (SR), and 0.33 μM μM (SC-1). KW-2478 also inhibits the transcription of c-Maf and Cyclin D1 genes by mainly suppressing the function of Cdk9.(In Vivo):KW-2478 (25-200 mg/kg, i.v.) inhibits tumor growth in combined immunodeficiency (SCID) mice bearing NCI-H929 cells, without body weight loss. KW-2478 (100 mg/kg, i.v.) causes degradation of the Hsp90 client proteins (IGF-1Rβ, c-Raf-1, Cdk9) levels and dephosphorylated Erk1/2 proteins in NCI-H929 tumors of mice.

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Key Properties

CAS Number819812-04-9
MW574.66
Purity>98% (HPLC)
FormulaC30H42N2O9
SMILESCCc1c(O)cc(O)c(C(=O)c2cc(OC)c(OCCN3CCOCC3)cc2)c1CC(=O)N(CCOC)CCOC
Target5-HT Receptor
SolubilityDMSO : ≥ 83.3 mg/mL; 144.96 mM

Bioactivity

In Vivo
KW-2478 (25-200 mg/kg, i. v.) inhibits tumor growth in combined immunodeficiency (SCID) mice bearing NCI-H929 cells, without body weight loss. KW-2478 (100 mg/kg, i. v.) causes degradation of the Hsp90 client proteins (IGF-1Rβ, c-Raf-1, Cdk9) levels and dephosphorylated Erk1/2 proteins in NCI-H929 tumors of mice.
In Vitro
KW-2478 is an inhibitor of Hsp90, with an IC50 of 3.8 nM for Hsp90α. KW-2478 shows anti-proliferative activity against multiple myeloma (MM) and non-Hodgkin’s lymphoma (NHL), with GI50s of 0.30 μM (OPM-2/GFP), 0.34 μM (KMS-11), 0.39 μM (RPMI 8226), 0.12 μM (NCI-H929), 0.36 μM (Raji), 0.098 μM (SR), and 0.33 μM μM (SC-1). KW-2478 also inhibits the transcription of c-Maf and Cyclin D1 genes by mainly suppressing the function of Cdk9.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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  • KW-2478 [orb1300660]

    99.52% (May vary between batches)

    819812-04-9

    574.66

    C30H42N2O9

    1 mg, 2 mg, 5 mg, 10 mg, 25 mg, 100 mg, 1 ml x 10 mM (in DMSO), 50 mg
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KW-2478 (orb1223043)

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Available Sizes

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200 mg
500 mg
2 mg
$ 150.00
5 mg
$ 250.00
10 mg
$ 350.00
25 mg
$ 610.00
50 mg
$ 870.00
100 mg
$ 1,160.00