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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
CH5138303 (CH 5138303; CH-5138303) is a novel, potent, orally boavailable HSP90 (Heat Shock Protein 90) inhibitor with potential anticancer activity. It inhibits HSP90 with a Kd of 0.48 nM. CH5138303 exhibits high in vivo antitumor efficacy in Human NCI-N87 gastric cancer xenograft model.
ln Vitro |
CH5138303 has antifungal efficacy against azole-resistant C when administered in conjunction with FLC. albicans, as evidenced by its 0.500 FICI (fractional inhibitory concentration index)[2].
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ln Vivo |
With a median effective dose (ED50) of 3.9 mg/kg and a tumor growth inhibition (TGI) of 136%, CH5138303 (SCID mice carrying NCI-N87 cells, 0-50 mg/kg, Orally, once daily for 11 days) has strong anticancer activity without causing a discernible decrease of body weight[1].
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Animal Protocol |
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References |
[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. |
Molecular Formula |
C19H18CLN5O2S
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Molecular Weight |
415.9
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CAS # |
959763-06-5
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Related CAS # |
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SMILES |
O=C(N)CCCSC1=NC(N)=NC(C2=C3C(C(COC4)=CC=C3)=C4C=C2Cl)=N1
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InChi Key |
VIGHQZSTZWNWFA-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H18ClN5O2S/c20-13-7-11-9-27-8-10-3-1-4-12(15(10)11)16(13)17-23-18(22)25-19(24-17)28-6-2-5-14(21)26/h1,3-4,7H,2,5-6,8-9H2,(H2,21,26)(H2,22,23,24,25)
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Chemical Name |
4-((4-amino-6-(5-chloro-1,3-dihydrobenzo[de]isochromen-6-yl)-1,3,5-triazin-2-yl)thio)butanamide
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.