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ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.

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ATM-3507

ATM-3507 構造式

CAS 番号 : 1861449-70-8

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 436 在庫あり
Solution
10 mM * 1 mL in DMSO USD 436 在庫あり
Solid
5 mg $324 在庫あり
10 mg $485 在庫あり
25 mg $824 在庫あり
50 mg $1200 在庫あり
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製品説明

ATM-3507 is a potent tropomyosin inhibitor with IC50s from 3.83-6.84 μM in human melanoma cell lines.

IC50 & Target

IC50: 3.83-6.84 μM (tropomyosin, in human melanoma celllines)[1].

体外実験

The cell lines differ in their relative expression of Tpm3.1 as well as in the expression of other isoforms. After determing the IC50 concentrations for TR100 and ATM-3507 (CHLA-20: 4.99±0.45 μM, CHP-134: 3.83±0.67 μM, CHLA-90: 6.84±2.37 μM, SK-N-BE(2): 5.00±0.42 μM) in each of the neuroblastoma cell lines, combinations of tropomyosin inhibitors plus Vincristine are tested at levels of each drug alone that kill less than 50% of the neuroblastoma cells. The combinations of both tropomyosin inhibitors plus Vincristine are completely cytotoxic in CHLA-20 cells. All 4 cell lines show some degree of synergy as determined by the Chou–Talalay method. The effect is not limited to the vinca alkaloids as a similar combination efficacy using paclitaxel plus TR100 or ATM-3507[1].

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

体内実験

The maximal tolerance dose (MTD) for TR100 and ATM-3507 is 60 and 150 mg/kg, respectively. It is found that a significant inhibition of tumor growth and prolongation of animal survival using either combination compared with each monotherapy. The median survival of mice increased from 18 days for mice treated with ATM-3507 to more than 49 days for mice treated with the combination. It is also found that twice weekly intravenous administration of ATM-3507 also show combination efficacy. The impact of each treatment or the combination on body weight is minimal. Drug levels are measured following the intravenous administration of ATM-3507 at 30 mg/kg in Balb/c mice (n=3 per time point). The mean half-life of ATM-3507 is 5.01 hrs for the terminal elimination phase. The mean AUC0-t in the plasma is 14,548 ng/h/mL. The Cmax of ATM-3507 is 5,758 ng/mL and the the t1/2 is 5.01 h. The observed plasma clearance and volume of distribution at steady state of ATM-3507 is 33.8 mL/min/kg and 7.23 L/kg, respectively[1].

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

分子量

611.79

分子式

C37H46FN5O2

CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC=CC(OC2=CC3=C(N(CCCN4CCN(C)CC4)C(C)=C3C)C=C2)=C1)N5CCN(CCC6=CC=C(F)C=C6)CC5

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶剤 & 溶解度
体外: 

DMSO : 33.33 mg/mL (54.48 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 1.6345 mL 8.1727 mL 16.3455 mL
5 mM 0.3269 mL 1.6345 mL 3.2691 mL
10 mM 0.1635 mL 0.8173 mL 1.6345 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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純度とドキュメンテーション

純度: 98.12%

参考文献
細胞実験
[1]

The 4 melanoma cell lines CHLA-20, CHLA-90, SK-N-BE(2) and CHP-134 are cultured at 37°C in a humidified incubator at 5% CO2 and supplemented 100 U/mL penicillin and 100 mg/mL streptomycin. Cells are plated in 96-well plates at 2000-4000 cells per well, incubated at 37°C overnight and then treated with various concentrations of TR100/ATM-3507 (0.1-2.5 μM) alone, TR100 and ATM-3507 plus various chemotherapy drugs. The cell viability is performed on day 3-5. For the dosing schedule optimization experiment, TR100 or Vincristine is added at day 1 with the other being added at day 2 or both TR100 and Vincristine are added on day 1 and plates are read at day 5. Results are presented as percentage of survival cells compared with controls. All cell viability assays are run in quadruplicate and the data shown are representative of at least 2 independent experiments[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[1]

Mice[1]
Female athymic nude mice (age 4-6 weeks) are used. Mice are subcutaneously injected with 5.0×106 CHLA-20 cells in a 150 mL mix of PBS and Matrigel (2:1). ATM-3507 and TR100 are formulated at 15 mg/mL in 30% sulfobutyl-ether-b-cyclodextrin sodium salt (SBECD). Vincristine is dissolved in H2O at 0.125 mg/kg. When the tumors reached volumes of 200-400 mm3, mice are randomized into the study groups. Animals are followed until the animal reached endpoint criteria. Tumor size is measured using digital calipers twice per week and tumor volume is calculated. Mice are also weighed and observed twice per week for signs of endpoint condition. Mice that demonstrate signs of toxicity or reach endpoint criteria are humanely euthanized by CO2 as phyxiation and subjected to cervical dislocation as the secondary method of euthanasia[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献

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 (protect from light). 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 1.6345 mL 8.1727 mL 16.3455 mL 40.8637 mL
5 mM 0.3269 mL 1.6345 mL 3.2691 mL 8.1727 mL
10 mM 0.1635 mL 0.8173 mL 1.6345 mL 4.0864 mL
15 mM 0.1090 mL 0.5448 mL 1.0897 mL 2.7242 mL
20 mM 0.0817 mL 0.4086 mL 0.8173 mL 2.0432 mL
25 mM 0.0654 mL 0.3269 mL 0.6538 mL 1.6345 mL
30 mM 0.0545 mL 0.2724 mL 0.5448 mL 1.3621 mL
40 mM 0.0409 mL 0.2043 mL 0.4086 mL 1.0216 mL
50 mM 0.0327 mL 0.1635 mL 0.3269 mL 0.8173 mL
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一般には略語で表示されます:C1V1 = C2V2

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    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.

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製品名:
ATM-3507
製品番号:
HY-100948
数量:
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