CH5138303( CH5138303 | CH-5138303 | CH 5138303 )

Catalog No. M19285 CAS No. 959763-06-5

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

CH5138303
Note

Research use only, not for human use.
Brief Description

CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
Description

CH5138303 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%).
In Vitro

When used in combination with FLC, CH5138303 shows antifungal activitiy against azole-resistant C. albicans, with a FICI (fractional inhibitory concentration index) of 0.500.
In Vivo

CH5138303 (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.
Synonyms

CH5138303 | CH-5138303 | CH 5138303
Pathway

Endocrinology/Hormones
Target

Reductase
Recptor

HSP90α
Research Area

Cancer
Indication

——

CAS Number

959763-06-5
Formula Weight

415.9
Molecular Formula

C19H18ClN5O2S
Purity

>98% (HPLC)
Solubility

——
SMILES

NC(=O)CCCSC1=NC(N)=NC(=N1)C1=C(Cl)C=C2COCC3=CC=CC1=C23
Chemical Name

4-((4-amino-6-(5-chloro-1,3-dihydrobenzo[de]isochromen-6-yl)-1,3,5-triazin-2-yl)thio)butanamide

1. Suda A, et al. Bioorg Med Chem. 2014, 22(2), 892-905.

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