959763-06-5
Chemical Structure
CH5138303
- CAS No.: 959763-06-5
- Formula:C19H18ClN5O2S
- Molecular Weight:415.90
IUPAC Name: 4-((4-amino-6-(5-chloro-1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazin-2-yl)thio)butanamide
InChIKey: VIGHQZSTZWNWFA-UHFFFAOYSA-N
SMILES: O=C(N)CCCSC1=NC(N)=NC(C2=C(Cl)C=C3C4=C2C=CC=C4COC3)=N1
Biological Activity: CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model[1][2].
| Cat. No. | 상품명 | Purity | 제품 설명 | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
CH5138303 | 99.04% | CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Atsushi Suda, et al. Design and synthesis of 2-amino-6-(1H,3H-benzo[de]isochromen-6-yl)-1,3,5-triazines as novel Hsp90 inhibitors. Bioorganic & Medicinal Chemistry. 15 January 2014;22(2):892-905.
- [2]. Yuan R, et al. Effects of Hsp90 Inhibitor Ganetespib on Inhibition of Azole-Resistant Candida albicans. Front Microbiol. 2021 May 20;12:680382. [Content Brief]
Keywords
