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Hepsulfam

Catalog No. T15472 CAS 96892-57-8

Synonyms: NCI 329680, ZINC01574758

Hepsulfam is an anticancer agent. It also displays excellent antileukemic activity (a median IC50: 0.91 μg/mL in a panel of different tumors).

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Hepsulfam, CAS 96892-57-8

Pack Size	Availability	Price/USD
2 mg	5 days	$ 140.00
25 mg	6-8 weeks	$ 766.00
50 mg	6-8 weeks	$ 996.00
100 mg	6-8 weeks	$ 1,540.00
1 mL * 10 mM (in DMSO)	5 days	$ 316.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	Hepsulfam is an anticancer agent. It also displays excellent antileukemic activity (a median IC50: 0.91 μg/mL in a panel of different tumors).
Targets&IC50	Tumors:0.91 μg/ml
In vitro	Hepsulfam exhibits greater toxicity towards L1210 leukemia cells compared to busulfan, its structural analogue, by inducing DNA interstrand cross-links in these cells, an effect not seen with busulfan. This compound also shows increased cytotoxicity against human leukemia (111-60 and K562) and colon carcinoma (BE and HT-29) cell lines relative to busulfan, correlating with higher levels of DNA interstrand cross-links. In a clonogenic assay, hepsulfam demonstrated activity in 22% (8 out of 37) of tumors at a concentration of 1.0 μg/mL. Additionally, it significantly affects human bone marrow cells (CFU-GM) from healthy donors, indicating its potency. In vitro evaluations reveal hepsulfam's superior activity, notably against non-small cell lung cancer, even at tenfold reduced concentrations and extended exposure times (12 h), underscoring its potential therapeutic benefit in a broad spectrum of cancers.
In vivo	The preclinical activity of hepsulfam shows a possible role of this compound in the treatment of solid human malignancies. Hepsulfam demonstrates superior in vivo activity in a large cell lung cancer xenograft and a gastric carcinoma model. The increased bone marrow toxicity of hepsulfam as compared with the busulfan might be critical for further clinical application[1].

Synonyms	NCI 329680, ZINC01574758
Molecular Weight	290.36
Formula	C7H18N2O6S2
CAS No.	96892-57-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Berger DP, et al. Preclinical activity of hepsulfam and busulfan in solid human tumor xenografts and human bone marrow. Anticancer Drugs. 1992 Oct;3(5):531-9. 2. Pacheco DY, et al. Mechanisms of toxicity of hepsulfam in human tumor cell lines. Cancer Res. 1990 Dec 1;50(23):7555-8.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid 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 master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Hepsulfam 96892-57-8 Others NCI 329680 ZINC-01574758 ZINC01574758 ZINC 01574758 NCI329680 NCI-329680 inhibitor inhibit

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