KW-2478
KW-2478
CAS: 819812-04-9
Molecular Formula: C30H42N2O9
KW-2478 - Names and Identifiers
KW-2478 - Physico-chemical Properties
| Molecular Formula | C30H42N2O9 |
| Molar Mass | 574.66 |
| Density | 1.209 |
| Storage Condition | -20℃ |
| In vitro study | KW-2478 inhibits the binding of bRD to Hsp90α with IC50 of 3.8 nM. KW-2478 degradates the Hsp90 client proteins, including FGFR3 and IGF-1Rβand c-Raf-1. KW-2478 reduces the level of phosphorylated Erk1/2. KW-2478 induces apoptosis by cleavage of PARP, a substrate of caspase-3 In U266 cells,. KW-2478 has Time dependency of antiproliferative activity consecutive drug exposure for at least 12 hours is necessary to to exert potent antitumor activity. KW-2478 downregulates the translocation products of IgH locus. KW-2478 inhibits the transcription of c-Maf and cyclin D1 genes by mainly suppressing the function Cdk9. KW-2478 has potent and broad growth inhibitory activities against various cell lines, KW-2478 inhibites cancer cell growth in all cell lines, with EC50 of 101-252 nM, 81.4-91.4 nM and 120-622 nM for B- cell lymphoma, mantle cell lymphoma and multiple myeloma. KW-2478 also show pot growth activity in primary CLL and NHL cells with EC50 of 40-170 nM and 200-400 nM. No. KW-2478 inhibited the binding of bRD to Hsp90α with an IC50 of 3.8 nM. KW-2478 degrades Hsp90 receptor proteins, including FGFR3,IGF-1Rβ and c-Raf-1. KW-2478 decreased the level of phosphorylated Erk1/2. In U266 cells, KW-2478 induced apoptosis by cleavage of PARP, a substrate for caspase-3. KW-2478 has time-dependent anti-proliferative activity requiring continuous drug exposure for at least 12 hours to exert potent anti-tumor activity. KW-2478 down regulated the translocation product of IgH site. KW-2478 inhibits the transcription of c-Maf and cyclin D1 genes by mainly inhibiting the function of cdk9. KW-2478 has potent and extensive inhibitory activity against various cell lines, KW-2478 inhibits cancer cell growth in all cell lines, with EC50 of 101-252 nM for B- cell lymphoma, mantle cell lymphoma, and multiple myeloma, respectively, 81.4-91.4 nM and 120-622 nM. KW-2478 also exhibited potent growth inhibitory activity in primary CLL and NHL cells with EC50 of 40-170 nM and 200-400, respectively nM. |
| In vivo study | KW-2478 suprises tumor growth and induces the degradation of client proteins in tumors in NCI-H929 s.c. incultural model at doses of 100 mg/kg or more. KW-2478 reductions both serum M protein and MM tumor burden in the bone marrow in OPM-2/GFP I. v. Inculated mouse model at doses of 100 mg/kg. In a model inoculated subcutaneously NCI-H929, KW-2478 inhibited tumor growth and induced receptor protein degradation in tumors at a dose of 100 mg/kg or higher. In a OPM-2/GFP intravenous vaccination mouse model, KW-2478 reduced serum M protein and MM tumor burden in bone marrow at a dose of 100 mg/kg. |
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CAS: 819812-04-9
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CAS: 819812-04-9
Tel: 18301782025
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Mobile: 18021002903
QQ: 3008007409
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Product Name: KW-2478 Visit Supplier Webpage Request for quotation
CAS: 819812-04-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 819812-04-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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