[CAS NO. 959763-06-5] CH5138303
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PRODUCTS SPECIFICATIONS [959763-06-5]
Catalog
SLK-S7340
Brand
Selleck
CAS
959763-06-5
DESCRIPTION [959763-06-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 415.9 |
| Molecular Formula | C19 H18 Cl N5 O2 S |
| SMILES | O=C(N)CCCSC1=NC(N)=NC(C2=C3C(C(COC4)=CC=C3)=C4C=C2Cl)=N1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4044 mL | 12.0221 mL | 24.0442 mL |
| 5 mM | 0.4809 mL | 2.4044 mL | 4.8088 mL |
| 10 mM | 0.2404 mL | 1.2022 mL | 2.4044 mL |
| 50 mM | 0.0481 mL | 0.2404 mL | 0.4809 mL |
Description
CH5138303 is an orally available inhibitor with of 0.48 nM.
Targets
| HSP90α [1] (Cell-free assay) |
| 0.48 nM(Kd) |
In vitro
CH5138303 shows high affinity to Hsp90αand potent cell growth inhibitory activity against an HCT116 colorectal cancer cell line and an NCI-N87 gastric cancer cell line with IC50 of 98 nM and 66 nM, respectively. [1] Besides, CH5138303 also demonstrates liver microsomal stability.
In vivo
CH5138303 (50 mg/kg p.o.) displays high oral bioavailability in mice and produces potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model.
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