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Hepsulfam  (Synonyms: NCI 329680; ZINC01574758)

Cat. No.: HY-U00095 Purity: 99.31%
COA Handling Instructions

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Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.

For research use only. We do not sell to patients.

Hepsulfam Chemical Structure

Hepsulfam Chemical Structure

CAS No. : 96892-57-8

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 287 In-stock
Solution
10 mM * 1 mL in DMSO USD 287 In-stock
Solid
1 mg USD 90 In-stock
5 mg USD 180 In-stock
10 mg USD 306 In-stock
20 mg USD 488 In-stock
50 mg USD 976 In-stock
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Hepsulfam Related Antibodies

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  • Biological Activity

  • Protocol

  • Purity & Documentation

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Description

Hepsulfam (NCI 329680; ZINC01574758) is a anticancer agent that shows excellent antileukemic activity with an median IC50 of 0.91 μg/mL in a panel of different tumors.

IC50 & Target

IC50: 0.91 μg/mL (Tumors)[1]
In Vitro

At a concentration of 1.0 μg/mL, hepsulfam is active in eight of 37 tumors (22%) in the clonogenic assay. Hepsulfam demonstrates a clear in vitro toxicity to human bone marrow cells (CFU-GM) from healthy donors. Evaluation of equitoxic concentrations in vitro reveals a higher activity of hepsulfam, especially in non-small cell lung cancer[1]. Hepsulfam is more toxic to L1210 leukemia cells than is busulfan, its structural homologue . Consistent with the difference in toxicity, hepsulfam induces DNA interstrand cross-links in L1210 mouse leukemia cells, whereas busulfan does not. Hepsulfam is more cytotoxic to two human leukemia cell lines (111-60 and K562) and to two human colon carcinoma cell lines (BE and HT-29) than is busulfan. As in 11210 cells, hepsulfam induces a higher level of DNA interstrand cross-links than busulfan. Hepsulfam is also more cytotoxic to the human leukemia cell lines when the concentrations are reduced 10-fold and the duration of drug exposure is increased to 12 h[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Hepsulfam Related Antibodies
In Vivo

Hepsulfam demonstrates superior in vivo activity in a large cell lung cancer xenograft and a gastric carcinoma model. The preclinical activity of hepsulfam suggests a possible role of this compound in the treatment of solid human malignancies. However, the increased bone marrow toxicity of hepsulfam as compared with busulfan might be critical for further clinical application[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

290.36

Formula

C7H18N2O6S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(OCCCCCCCOS(=O)(N)=O)(N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (344.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4440 mL 17.2200 mL 34.4400 mL
5 mM 0.6888 mL 3.4440 mL 6.8880 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.31%

COA (242 KB) HNMR (133 KB) LCMS (256 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

HL-60 or K562 leukemia cells (1x106/mL) are treated with various concentrations of hepsulfam for 2, 3,6, 9, or 12 h at 37°C. The concentration of DMSO in either control or treated cells is never greater than 2% (v/v). Following drug exposure, the cells are ished by centrifugation in RPMI 1640 medium and resuspended in fresh medium. Following this ish, cells are either assayed immediately for DNA damage by alkaline elution or incubated at 37°C for various periods before assay. BE and HT-29 human colon carcinoma cells are processed for alkaline elution analysis or cytotoxicity assays[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4440 mL 17.2200 mL 34.4400 mL 86.1000 mL
5 mM 0.6888 mL 3.4440 mL 6.8880 mL 17.2200 mL
10 mM 0.3444 mL 1.7220 mL 3.4440 mL 8.6100 mL
15 mM 0.2296 mL 1.1480 mL 2.2960 mL 5.7400 mL
20 mM 0.1722 mL 0.8610 mL 1.7220 mL 4.3050 mL
25 mM 0.1378 mL 0.6888 mL 1.3776 mL 3.4440 mL
30 mM 0.1148 mL 0.5740 mL 1.1480 mL 2.8700 mL
40 mM 0.0861 mL 0.4305 mL 0.8610 mL 2.1525 mL
50 mM 0.0689 mL 0.3444 mL 0.6888 mL 1.7220 mL
60 mM 0.0574 mL 0.2870 mL 0.5740 mL 1.4350 mL
80 mM 0.0431 mL 0.2153 mL 0.4305 mL 1.0763 mL
100 mM 0.0344 mL 0.1722 mL 0.3444 mL 0.8610 mL
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Hepsulfam Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hepsulfam96892-57-8NCI 329680 ZINC01574758NCI329680NCI-329680ZINC01574758ZINC 01574758ZINC-01574758OthersInhibitorinhibitorinhibit

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