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CH5138303
CAS No. 959763-06-5
CH5138303( CH5138303 | CH-5138303 | CH 5138303 )
Catalog No. M19285 CAS No. 959763-06-5
CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 203 | In Stock |
|
| 10MG | 324 | In Stock |
|
| 25MG | 584 | In Stock |
|
| 100MG | Get Quote | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameCH5138303
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NoteResearch use only, not for human use.
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Brief DescriptionCH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
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DescriptionCH5138303 is a novel and potent HSP90 inhibitor. CH5138303 showed high binding affinity for N-terminal Hsp90α (Kd=0.52nM) and strong in vitro cell growth inhibition against human cancer cell lines (HCT116 IC50=0.098μM, NCI-N87 IC50=0.066μM) and also displayed high oral bioavailability in mice (F=44.0%) and potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model (tumor growth inhibition=136%).
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In VitroWhen used in combination with FLC, CH5138303 shows antifungal activitiy against azole-resistant C. albicans, with a FICI (fractional inhibitory concentration index) of 0.500.
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In VivoCH5138303 (SCID mice bearing NCI-N87 cells, 0-50 mg/kg, Orally, once daily for 11 days) shows potent antitumor efficacy with TGI (tumor growth inhibition) of 136% and a median effective dose (ED50) of 3.9 mg/kg without significant loss of body weight.
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SynonymsCH5138303 | CH-5138303 | CH 5138303
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PathwayEndocrinology/Hormones
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TargetReductase
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RecptorHSP90α
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number959763-06-5
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Formula Weight415.9
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Molecular FormulaC19H18ClN5O2S
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Purity>98% (HPLC)
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Solubility——
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SMILESNC(=O)CCCSC1=NC(N)=NC(=N1)C1=C(Cl)C=C2COCC3=CC=CC1=C23
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Chemical Name4-((4-amino-6-(5-chloro-1,3-dihydrobenzo[de]isochromen-6-yl)-1,3,5-triazin-2-yl)thio)butanamide
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. Suda A, et al. Bioorg Med Chem. 2014, 22(2), 892-905.
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