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Letrozole

Letrozole Structure
CAS No.
112809-51-5
Chemical Name:
Letrozole
Synonyms
LETROZOL;FEMARA;LETRAZOLE;LetrozoleUsp28;Letrozole(FeMara);Letroz;etrozoL;Lelrozol;Lerozole;CGS-20267
CBNumber:
CB9286355
Molecular Formula:
C17H11N5
Molecular Weight:
285.3
MOL File:
112809-51-5.mol
MSDS File:
SDS
Modify Date:
2024/8/22 14:21:17
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Letrozole Properties

Melting point 181-183°C
Boiling point 563.5±60.0 °C(Predicted)
Density 1.21±0.1 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMSO: >50mg/mL
pka 1.52±0.11(Predicted)
form White powder
color white to off-white
Merck 14,5450
InChI InChI=1S/C17H11N5/c18-9-13-1-5-15(6-2-13)17(22-12-20-11-21-22)16-7-3-14(10-19)4-8-16/h1-8,11-12,17H
InChIKey HPJKCIUCZWXJDR-UHFFFAOYSA-N
SMILES C(C1=CC=C(C=C1)C#N)(C1=CC=C(C=C1)C#N)N1C=NC=N1
CAS DataBase Reference 112809-51-5(CAS DataBase Reference)

SAFETY

Risk and Safety Statements

Symbol(GHS) 
GHS08
Signal word  Warning
Hazard statements  H361fd-H373
Precautionary statements  P202-P260-P280-P308+P313-P405-P501
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  26-36
WGK Germany  3
RTECS  DI4957000
HS Code  2933997500

Letrozole price More Price(3)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich(India) PHR1540 Letrozole Pharmaceutical Secondary Standard; Certified Reference Material 112809-51-5 1G ₹9926.53 2022-06-14 Buy
Sigma-Aldrich(India) L6545 Letrozole ≥98% (HPLC) 112809-51-5 10MG ₹10532.73 2022-06-14 Buy
Sigma-Aldrich(India) L6545 Letrozole ≥98% (HPLC) 112809-51-5 50MG ₹42639.68 2022-06-14 Buy
Product number Packaging Price Buy
PHR1540 1G ₹9926.53 Buy
L6545 10MG ₹10532.73 Buy
L6545 50MG ₹42639.68 Buy

Letrozole Chemical Properties,Uses,Production

Description

Letrozole, also known as Femara, is an orally active aromatase inhibitor that works by competitively inhibiting aromatase. This inhibition prevents the conversion of androgens to estrogen (estrogen stimulates breast tissues and breast cancer reoccurrence) and gonadal steroidogenesis. It can be used for the treatment of breast cancer that is hormonally-responsive or has an unknown receptor status in postmenopausal women. Besides this, Letrozole also has some off-label use such as ovarian stimulation, pretreatment of termination of pregnancy, treatment of gynecomastia, treatment of endometriosis, and promoting spermatogenesis for male patients of nonobstructive azoospermia.

Chemical Properties

white to light yellow crystal

Uses

Letrozole has been used:

  • in organoid growth assay to determine its inhibitory capacity(48)
  • to investigate steroid receptor coactivator-1 (SRC-1) mediated endogenous estrogen regulation of hippocampal PSD-95(49)
  • to determine its effects on tumor-induced hyperalgesia(50)
  • for hormonal manipulation in rats(51)
  • to study its effects on lipocalin-2 (Lcn2)(52)
  • to determine its effects on mechanical hyperalgesia and aromatase expression(53)

General Description

Letrozole, 4,4'-(1H-1,2,4-triazol-1-ylmethylene)dibenzonitrile (Femara), is used for most of thesame indications as anastrozole. It reduces concentrations ofestrogens by 75% to 95%, with maximal suppressionachieved within 2 to 3 days. Letrozole is specific for aromataseinhibition, with no additional effects on adrenal corticoidbiosynthesis. CYPs 3A4 and 2A6 are involved in themetabolism of letrozole to the major carbinol metabolite,which is inactive. The loss of the triazole ring, which is involvedin coordination of the heme iron, would explain theloss of activity. Letrozole strongly inhibits CYP2A6 invitro, with moderate inhibition of CYP2C19. The effect ofthis in vitro inhibition on the pharmacokinetics of coadministereddrugs is unknown. Tamoxifen reduces the levels ofletrozole significantly if they are used together, so combinationtreatment with these agents is not recommended.

Biological Activity

Letrozole is a potent, cell-permeable inhibitor of aromatase (IC50 = 2 nM). It inhibits proliferation of estrogen receptor-positive (ER+) MCF-7 cells when used alone at concentrations ranging from 0.1 to 100 nM and when used at a concentration of 10 nM in combination with testosterone or 4-androstene-3,17-dione. It also reduces matrix metalloproteinase-2 (MMP-2) and MMP-9 levels in MCF-7 cells when used at a concentration of 10 nM. Letrozole (10 μg per day) reduces tumor growth in an MCF-7Ca ovariectomized-mouse xenograft model. Formulations containing letrozole have been used in the treatment of postmenopausal breast cancer.

Mechanism of action

Inhibition of arom atase by letrazole is competitive and highly specific , with no effect on enzymes that are responsible for the production of glucocorticosteroids and mineralocorticosteroids. This agent is significantly more effective than tamoxifen in treating horm one-dependent cancer.

Clinical Use

Femara was launched in France and the UK for second-line treatment of advanced breast cancer. Letrazole can be synthesized in two steps from 4- bromomethyl-benzonitrile with 1,2,4-triazole and is a third generation aromatase inhibitor. It is a highly specific inhibitor of P450arom which prevents the conversion of androstenedione to estrone. The reduction of plasma estrogen was immediate and long lasting. This is accomplished with no inhibition of other steroid biosynthesis making it the most selective aromatase inhibitor tested. Letrazole has remarkable antitumor activity, is well tolerated and has no toxic side effects. It is 10,000 times more potent than aminoglutethimide, in vivo, the first well established aromatase inhibitor.

References

https://www.drugbank.ca/drugs/DB01006
https://en.wikipedia.org/wiki/Letrozole

Letrozole Preparation Products And Raw materials

Raw materials

Potassium tert-butoxide 4-fluorobenzonitrile 3-Amino-5-mercapto-1,2,4-triazole 4-Cyanobenzyl bromide 1H-1,2,4-Triazole-3-carboxylic acid
3-Amino-1,2,4-Triazole 1,2,4-Triazole
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Preparation Products

Letrozole Suppliers

Global( 718)Suppliers
Supplier Tel Country ProdList Advantage Inquiry
Jigs Chemical ltd +919099003427 Gujarat, India 239 58 Inquiry
SGMR PHARMACEUTICALS PVT LTD +91-9032001889 +91-9032001889 Telangana, India 83 58 Inquiry
USV Pvt Ltd +91-2267861111 +91-2225564048 Maharashtra, India 36 58 Inquiry
Apotex Pharmachem India Pvt Ltd +91-8022891034 +91-8022891000 Karnataka, India 109 58 Inquiry
Cipla Ltd +912224826000 Maharashtra, India 133 58 Inquiry
Mascot Industries Pvt., Ltd. +91-9825849755 +91-9825849755 Ahmedabad, India 16 58 Inquiry
Basil Drugs AND Pharmaceuticals Pvt Ltd +91-2249700250 +91-9619320820 Mumbai, India 108 58 Inquiry
NATCO Pharma Limited +91-9849511345 +91-9866005199 Hyderabad, India 24 58 Inquiry
Gland Chemicals Pvt Ltd +91-9492733833 +91-9346729196 Telangana, India 16 58 Inquiry
Zydus Lifesciences Ltd. +91-0265-2315243 +91-6358895661 Gujarat, India 89 58 Inquiry
Supplier Advantage
Jigs Chemical ltd 58
SGMR PHARMACEUTICALS PVT LTD 58
USV Pvt Ltd 58
Apotex Pharmachem India Pvt Ltd 58
Cipla Ltd 58
Mascot Industries Pvt., Ltd. 58
Basil Drugs AND Pharmaceuticals Pvt Ltd 58
NATCO Pharma Limited 58
Gland Chemicals Pvt Ltd 58
Zydus Lifesciences Ltd. 58

Related articles

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Letrozole Spectrum

Letrozole(112809-51-5)1HNMR

112809-51-5(Letrozole)Related Search:

5-Methyl-1H-benzotriazole Chlorodimethylphenylsilane Tolyltriazole 1,2,4-Triazole 1H-Benzotriazole
Ribavirin 1-CHLOROMETHYL-1H-1,2,4-TRIAZOLE 4-(1H-1,2,4-Triazol-1-ylmethyl)benzonitrile 4,4',4 -METHYLIDENETRISBENZONITRILE(IMPURITY OF LETROZOLE),4,4’,4”-Methyledenetrisbenzonitrile ( Impurity of Letrozole ) Ibandronate sodium monohydrate
Irinotecan hydrochloride trihydrate LetrozoleN-Oxide 4,4'-(4H-1,2,4-TRIAZOL-4-YLMETHYLENE)BIS BENZONITRILE 4-((4-broMophenyl)(1H-1,2,4-triazol-1-yl)Methyl)benzonitrile (S)-1-(4-CYANOPHENYL)ETHANAMINE
4,4'-(1-METHYLENE) BIS-BENZONITRILE 5-Methyl-1,3-benzenediacetonitrile (R)-1-(4-CYANOPHENYL)ETHANAMINE
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Letrozole99% CGS-20267, Femara letrozolex Lelrozol 1-[BIS(4-CYANOPHENYL)METHYL]-1,2,4-TRIAZOLE 4,4'-(1H-1,2,4-Triazol-1-ylmethylene)dibenzonitrile 4,4'-(1H-1,2,4-Triazole-1-ylmethylene)bisbenzonitrile 4,4'-[(1H-1,2,4-Triazole-1-yl)methylene]dibenzonitrile Letrozole (200 mg) 4-[(4-cyanophenyl)(1H-1,2,4-triazol-1-yl)Methyl]benzonitrile 20MG/50MG/1KG Lerozole Letrof L Lil Letroz Letrozole###112809-51-5 Aromatase Inhibitor II, Letrozole Letrozol Tablets CGS-20267 LETROZOLE Letrozole 4,4'-(1H-1,2,4-Triazol-1-ylmethylene)bisbenzonitrile 4,4'-(1H-1,2,4-TRIAZOL-1-YLMETHYLENE) BIS-BENZONITRILE Letrazole(Femara) To letrozole Aromatase Inhibitor II, Letrozole - CAS 112809-51-5 - Calbiochem Letrozole powder Letrozole CRS Letrozole,98% etrozoL Benzonitrile, 4,4'-(1H-1,2,4-triazol-1-ylmethylene)bis- Top quality Letrozole 4,4'-(1,2,4-Triazol-1-ylmethylene)dibenzonitrile Letrozole USP/EP/BP LetrozoleAPI & intermediates Letrozole (CGS 20267) Letrozole (Femara, LET)-1 gram(57) LetrozoleQ: What is Letrozole Q: What is the CAS Number of Letrozole Q: What is the storage condition of Letrozole Q: What are the applications of Letrozole Letrozole (1356971) LetrozoleUsp28 LETRAZOLE Letrozole(FeMara) FEMARA LETROZOL Ethanol,2-[(5-bromo-6-pyrimidinyl)oxy]- Femara, Letrozole Letrozole CAS 112809-51-5 Letrozole / Letrazole / Femara Letrozol Femara 4,4'-((1H-1,2,4-Triazol-1-yl)methylene)dibenzonitrile Latrozole 112809-51-5 112809-51-9 C17H11N5 2853 Anti-cancer&immunity Aromatics Heterocycles APIs Antibiotics