Letrozole

製品コードS1235 別名:CGS 20267

Letrozole化学構造

分子量(MW):285.3

Letrozole is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM.

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JPY 79680.00 あり
JPY 16102.00 あり
JPY 28220.00 あり
JPY 78020.00 あり

カスタマーフィードバック(4)

  • Effect of aromatase inhibitor letrozole on cellular proliferation marker Ki-67 expression in LNCaP tumor xenografts. A, Ki-67 immunostaining in transverse sections of xenograft tumors from C, C+T, C+T+D, C+T+L, and C+T+D+L mice 2 days after testosterone replacement. Panel B, Quantification of Ki-67–positive cells in LNCaP tumors at day 2 post testosterone replacement. Error bars represent SEM. Number of animals in each group is shown in parentheses. ***, P <.0001.

    Endocrinology 2013 154, 2296-307. Letrozole purchased from Selleck.

    Letrozole impairs object recognition and object placement memory consolidation. (A) Mice receiving bilateral dorsal hippocampal infusion of vehicle (n = 13), but not 0.005 μg (n = 9), 0.025 μg (n = 10), or 0.05 μg (n = 12) letrozole, immediately after training spent significantly more time with the novel object 24 h after training relative to chance (dashed line at 15 s). Vehicle-infused mice also spent significantly more time with the novel object than mice infused with 0.025 or 0.05 μg letrozole. These data suggest that the 0.025 and 0.05 μg doses of letrozole blocked object recognition memory consolidation. (B) Mice receiving bilateral dorsal hippocampal infusions of vehicle (n = 12) or 0.005 μg (n = 9) letrozole, but not 0.025 μg (n = 9) or 0.05 μg (n = 9) letrozole, immediately after training spent significantly more time than chance (*p < 0.05) with the moved object 4 h after training. Vehicle-infused mice also spent significantly more time with the moved object than mice infused with 0.025 or 0.05 μg letrozole, suggesting that the 0.025 and 0.05 μg doses of letrozole also blocked spatial memory consolidation. This effect was limited to within the first 2–3 h after training, as mice receiving a bilateral infusion of vehicle (n = 11) or 0.025 μg letrozole (n = 10) 3 h after OR training (C), or 2 h after OP training (vehicle: n = 13; letrozole: n = 9) (D), spent significantly more time than chance with the novel object (*p < 0.05), suggesting that the memory-impairing effects of letrozole are specific to the consolidation period immediately after training. *p < 0.05, **p < 0.01, ***p < 0.001 relative to chance; #p < 0.05 for between-group differences measured by Tukey's post hoc tests.

    Horm Behav, 2016, 83:60-7. Letrozole purchased from Selleck.

  • Uterus from mice treated with Letrozole. (A) 13 weeks old aP2-Cre/ERαflox/flox mice treated with vehicle have swollen abdomen while littermates treated with Letrozole for 17 days looks normal (B). (C) Uterus from vehicle treated aP2-/ERαflox/flox mice with severe hydrometra. (D) Uterus from Letrozole treated aP2-Cre/ERαflox/flox mice looks normal.

    PLoS One 2014 9(1), e85581. Letrozole purchased from Selleck.

    Functional comparison of mono-cultured MCF7 cells and MCF7 cells co-cultured with CAFs before and after letrozole treatment. Cell invasion (a), migration (b), adhesion (c) and proliferation assays (d) revealed that MCF7 cells co-cultured with CAFs displayed increasing adhesion, invasion, migration and proliferation abilities compared with mono-cultured cells either with or without letrozole treatment. The invasion, migration and adhesion of co-cultured MCF7 cells were decreased after letrozole treatment (a–c). Letrozole had no effect on mono-cultured MCF7 cell migration, invasion, adhesion or proliferation (a–d). e–g Representative images of invasion, migration and adhesion assays (magnification: ×100). LET represents letrozole. MO and CO represents mono-cultured and co-cultured, respectively. Data are presented as the mean ± SD. *P < 0.05 and ***P < 0.001, as determined using the independent sample T test

    Med Oncol, 2016, 33(7):64. Letrozole purchased from Selleck.

製品安全説明書

Aromatase阻害剤の選択性比較

生物活性

製品説明 Letrozole is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM.
ターゲット
Aromatase [1]
(Cell-free assay)
0.07 nM-20 nM
体外試験

Letrozole potently inhibits aromatase derived from a variety of different sources including human placental microsomes, particulate fractions of human breast cancer, rat ovarian microsomes, MCF-7 cells transfected with aromatase (MCF-7Ca), JEG-3 human choriocarcinoma cells , CHO cells, hamster ovarian tissue, and particulate fractions of human breast cancer with IC50 of 11, 2, 7, 0.07, 0.07, 1.4, 20 and 0.8 nM. In the non-cellular systems, the IC50 of letrozole is calculated to be 1-13 nM. [1] Letrozole maximally inhibits estradiol production in vitro in LH-stimulated hamster ovarian tissue at 0.1 μM with an IC50 of 0.02 μM and does not significantly affect progesterone production up to 350 μM. In ACTH-stimulated rat adrenal tissue in vitro, aldosterone production is inhibited by with an IC50 of 210 μM. [2] Letrozole inhibits growth of the MCF-7 epithelial breast cancer cells in a dose-dependent way with IC50 of 1 nM. Inhibition can be observesed even at the very low concentrations tested (0.1 nM). Treatment of normal MCF-12A epithelial cells with letrozole did not affect their growth even when high letrozole concentrations (100 nM) or prolonged culture times. Letrozole (10 nM) significantly suppressed the stimulatory effects of 4-androstene-3,17-dione (100 nM) or testosterone (100 nM) on MCF-7 cell proliferation. Concurrent administration of 17-β-estradiol with letrozole (10 nM) decreased the stimulatory effect of the enzymatic activity of MMP-2 and - 9 released by estradiol. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MCF7a cells MlG2R5l1d3SxeHnjbZR6KGG|c3H5 Mlv6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHP2FiY3XscJMh\XiycnXzd4lv\yCWZYStc4ZnNTOkZYThTHNFOS2Dcn;tJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gWHNVNXO2aX31cIF1\WRiY3XscEBxem:uaX\ldoF1cW:wIH3lZZN2emWmIHHmeIVzKDFyIHThfZMtKEWFNUC9OIUuODZizszN NVPkdIIxOjJ7NUGwO|Q>
human JEG3 cells Mo\USpVv[3Srb36gZZN{[Xl? MWrJcohq[mm2aX;uJI9nKGG{b33heIF{\SCjY4Tpeol1gSCrbjDoeY1idiCMRVezJINmdGy|LDDJR|UxRTBwMECwPFkh|ryP NWr1VnRrOTh3OUCyO|I>
human MCF7 cells MkXtR5l1d3SxeHnjbZR6KGG|c3H5 NIjwR2c4OiCq NInjeZpEgXSxdH;4bYNqfHliYXfhbY5{fCCnc4Tyc4dmdi2mZYDlcoRmdnRiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvODB5IN88US=> Mon6NlQ{PDV2OEG=
human MDA-MB-435 cells M3[4O2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MojvOFghcA>? M2nFU2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1FSS2PQj20N|Uh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IIP1cIZwemixZHHtbY5mKEJiYYPzZZktKEeLNUC9NE4xPjdizszN MVGyNFk2ODh7OB?=
human IGROV1 cells MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYHGO|ZFPDhiaB?= MorQS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gTWdTV1ZzIHPlcIx{KGGodHXyJFQ5KGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDHTVUxRTBwMEm1JO69VQ>? NFLBdoczODl3MEi5PC=>
human MDA-MB-231 cells NXHJfIE2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWjH[IFnPDhiaB?= Ml3ZS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB2ODDodpMh[nlic4Xs[o9zcG:mYX3pcoUhSiCjc4PhfUwhT0l3ME2wMlE2KM7:TR?= NGLlVXgzODl3MEi5PC=>
human T47D cells MYHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVm1RXBIPDhiaB?= NFfHfolIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBVPDeGIHPlcIx{KGGodHXyJFQ5KGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDHTVUxRTBwNESg{txO NFzudpUzODl3MEi5PC=>
human MCF7 cells MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYW0PEBp M3\mZWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OC55IN88US=> M2fnOVIxQTVyOEm4
human OVCAR4 cells MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYC0PEBp MW\Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDPWmNCWjRiY3XscJMh[W[2ZYKgOFghcHK|IHL5JJN2dG[xcnjv[IFucW6nIFKgZZN{[XluIFfJOVA:OC56ODFOwG0> M123TFIxQTVyOEm4
human BT549 cells NWPxOolDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnXpOFghcA>? NITUbZpIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBDXDV2OTDj[YxteyCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygS2k2OD1yLki5JO69VQ>? MWCyNFk2ODh7OB?=
human SKOV3 cells NVPyb3NXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2LyS|Q5KGh? NUDrVFVPT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hW0uRVkOgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGdKPTB;MT6wPUDPxE1? MlzNNlA6PTB6OUi=
human NCI/ADR-RES cells MkS4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUS0PEBp NFzSTYhIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBPS0lxQVTSMXJGWyClZXzsd{Bi\nSncjC0PEBpenNiYomgd5Vt\m:{aH;kZY1qdmViQjDhd5NigSxiR1m1NF0yNjF4IN88US=> NUH2NJJ[OjB7NUC4PVg>
human MDA-N cells NGrsXXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml[1OFghcA>? NUjXeGZRT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV6gZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KHO3bH\vdohw\GGvaX7lJGIh[XO|YYmsJGdKPTB;MT62NUDPxE1? NGroW4czODl3MEi5PC=>
human OVCAR5 cells NHvVdZZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoTXOFghcA>? MmLoS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gU3ZESVJ3IHPlcIx{KGGodHXyJFQ5KGi{czDifUB{fWyob4Loc4RidWmwZTDCJIF{e2G7LDDHTVUxRTFwNkKg{txO NF\EVpUzODl3MEi5PC=>
human OVCAR8 cells MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MonKOFghcA>? M3LTO2dzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GUODDj[YxteyCjZoTldkA1QCCqcoOgZpkhe3WuZn;ybI9l[W2rbnWgRkBie3OjeTygS2k2OD12LkWg{txO M4rpbVIxQTVyOEm4

多くの細胞株試験データを見る場合、クリックしてください

体内試験 Letrozole inhibits aromatase in vivo with ED50 of 1-3 μg/kg p.o.. [2] Letrozole displays anti-endocrine effects. Letrozole inhibits androstenedione-induced uterine hypertrophy in immature rats with ED50 of 1-3 μg/kg. In the adult female rat, Letrozole (0.3-1 mg/kg daily p.o., 14 days) completely interrupts ovarian cyclicity and reduces uterine weight and serum estradiol (E2) concentrations to a similar extent to that seen after ovariectomy. [1] Letrozole induces dose-dependent regression of estrogen-dependent, 9,10-dimethylbenz-a-anthracene (DMBA)-induced mammary tumors in adult female rats. The ED50 for Letrozole is determined to be 10 - 30 µg/kg/day, with complete inhibition at a daily dose of 10 µg/day. [4] Letrozole produces dose-dependent inhibition of tumor growth of MCF-7 cells transfected with human aromatase gene (MCF-7Ca) implanted athymic nude mice, with complete inhibition at 20 mg/kg per day p.o.. [5]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[6]

+ 展開

Human placental aromatase activity:

The assay is performed in a total volume of 1 mL at 37 ℃. Unless otherwise noted, the incubation mixture contains 11 nM [4- 14C] androstene-3, 17-dione ([4- 14C]A), 24 mM NADPH (tetrasodium salt Type III), the appropriate concentrations of the desired inhibitor, and 120 μg of microsomal protein. The (4- 14C)A is added as a solution in 1.7% ethanol in 0.05 M potassium phosphate buffer (pH 7.4), so that the final concentration of ethanol does not exceed 0.02% (v/v). The reaction is started by the addition of enzyme and stopped after 20 min by the addition of 7 vol of ethyl acetate. The mixture is agitated on a vortex mixer and centrifuged at 600 g for 5 min. The aqueous phase is re-extracted with 7 vol of ethyl acetate, and the combined extracts are evaporated to dryness using an Evapo-Mix. Over 99% of the radio- active of [4- 14C] added is recovered using this extraction system. The residue obtained is dissolved in 150 μL acetone, and 100 μL aliquots are chromatographed for 65 min on thin-layer plates precoated with silica gel 60 using ethyl: acetate: isooctane (140:60, v/v; system A) or toluene: chloroform: methanol (70:140:20; system B). The radioactive zones of the plate are located with a Berthold LB 2760 thin-layer scanner. The radioactive estradiol (E2) and estrone (E1) neaks are identified by comparison with authentic standards. The corresponding bonding band of silica gel is transferred to vials containing 10 mL of scintillation fluid, and counted with a 6880 Liquid Scintillation system.
細胞試験:

[3]

+ 展開
  • 細胞株: Human breast cancer cells MCF-7
  • 濃度: ~100 nM
  • 反応時間: 1 days
  • 実験の流れ:

    Cells are seeded in duplicate at 5,000 to 10,000 cells per well in 24-well plates. The day after plating, different concentrations of Letrozole are added. At the end of incubation, cells are trypsinizated and placed in Isotone solution and counted immediately using a Coulter particle-counter.


    (参考用のみ)
動物試験:

[5]

+ 展開
  • 動物モデル: Human breast carcinoma xenografts MCF-7 with human aromatase gene (MCF-7Ca)
  • 製剤: 0.5% (w/v) solution of carboxymethylcellulos
  • 投薬量: 20 mg/kg/day
  • 投与方法: orally administered by gavage once every 2 days
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 57 mg/mL (199.78 mM)
Water Insoluble
Ethanol Insoluble
体内 順序で溶剤を入れること:
0.5% CMC Na
10mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。

化学情報

分子量 285.3
化学式

C17H11N5

CAS No. 112809-51-5
保管
別名 CGS 20267

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02941926 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis November 30, 2016 Phase 3
NCT00006174 Completed McCune Albright Syndrome|Polyostotic Fibrous Dysplasia|Precocious Puberty National Institute of Dental and Craniofacial Research (NIDCR)|National Institutes of Health Clinical Center (CC) August 3, 2000 Phase 1
NCT03007979 Not yet recruiting Breast Cancer|Breast Carcinoma|Cancer of Breast|Malignant Tumor of Breast Washington University School of Medicine February 28, 2017 Phase 2
NCT02907918 Not yet recruiting Breast Cancer|Cancer of Breast|Breast Carcinoma Washington University School of Medicine|Pfizer February 28, 2017 Phase 2
NCT01872260 Recruiting Breast Cancer Novartis Pharmaceuticals|Novartis October 22, 2013 Phase 1
NCT03008408 Not yet recruiting Malignant Neoplasms of Female Genital Organs|Endometrial Carcinoma M.D. Anderson Cancer Center|Novartis April 2017 Phase 2

技術サポート

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Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

Aromatase信号経路図

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID