1. Cell Cycle/DNA Damage
  2. Topoisomerase
  3. Namitecan

Namitecan (Synonyms: ST-1968)

Cat. No.: HY-14821 Purity: 98.11%
Handling Instructions

Namitecan is a potent topoisomerase I inhibitor, with antitumor property.

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

Namitecan Chemical Structure

Namitecan Chemical Structure

CAS No. : 372105-27-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 478 In-stock
Estimated Time of Arrival: December 31
1 mg USD 245 In-stock
Estimated Time of Arrival: December 31
5 mg USD 500 Get quote
10 mg USD 850 Get quote
50 mg USD 2550 Get quote
100 mg   Get quote  
200 mg   Get quote  

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Description

Namitecan is a potent topoisomerase I inhibitor, with antitumor property.

IC50 & Target[1]

Topoisomerase I

 

In Vitro

Namitecan and cetuximab cooperate in inhibiting EGFR expression. Namitecan induces a dose-dependent decrease in EGFR expression in the different cell lines[1]. ST1968 induces a comparable level of apoptosis in A431 and A431/TPT cells with IC50 of 0.21 and 0.29 μM[2].

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

In Vivo

Namitecan (10 mg/kg) in combination with cetuximab (1 mg/mouse) induces synergistic antitumor effects in SCC models as a function of EGFR gene copy number[1]. ST1968 (25 mg/kg) causes acceptable body weight loss and no toxic deaths. ST1968 produces a 100% complete response rate in the mice bearing the A431 tumor, and retains a relevant activity in the topotecan-resistant tumor[2].

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

Clinical Trial
Molecular Weight

434.44

Formula

C₂₃H₂₂N₄O₅

CAS No.

372105-27-6

SMILES

O=C1[[email protected]](O)(CC)C2=C(CO1)C(N3CC4=C(/C=N/OCCN)C5=CC=CC=C5N=C4C3=C2)=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 : 250 mg/mL (575.45 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3018 mL 11.5091 mL 23.0181 mL
5 mM 0.4604 mL 2.3018 mL 4.6036 mL
10 mM 0.2302 mL 1.1509 mL 2.3018 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

The antiproliferative activity is evaluated after 72 hours of drug exposure by cell counting. Drug concentrations able to inhibit cell proliferation by 50% (IC50) and 20% (IC20) are calculated from dose-response curves.

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

Animal Administration
[1]

To generate tumor xenografts, exponentially growing cells (A431 and A431/topotecan, 107 cells/mouse; SiHa 2.5 × 107 cells/mouse, Caski 107 cells/mouse) are s.c. injected into the mice flanks. For antitumor activity studies, groups of four/five mice bearing tumor implanted in both flanks are used. Tumor fragments are implanted on day 0, and tumor growth is followed by biweekly measurements of tumor diameters with a Vernier caliper. Tumor volume (TV) is calculated according to the formula TV (mm3) = d2 × D/2, in which d and D are the shortest and the longest diameter, respectively. Treatment starts 5 to 13 days after implant, when the tumors are just palpable, but established (TV = 80-90 mm3). Namitecan, irinotecan, and cetuximab are administered every fourth day for four times. Cetuximab is given 1 hour after each administration of the camptothecin.

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

References
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Keywords:

NamitecanST-1968ST1968ST 1968TopoisomeraseInhibitorinhibitorinhibit

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