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Lapatinib ditosylate monohydrate

Lapatinib ditosylate monohydrate structure

CAS No:
388082-78-8
Formula:
C29H26ClFN4O4S.2C7H8O3S.H2O
Chemical Name:
Lapatinib ditosylate monohydrate
Synonyms:
4-Quinazolinamine,N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-,4-methylbenzenesulfonate,hydrate (1:2:1);4-Quinazolinamine,N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-,bis(4-methylbenzenesulfonate),monohydrate;Lapatinib ditosylate monohydrate
Categories:
Specialty Chemicals

Description

Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].

Lapatinib ditosylate monohydrate Basic Attributes

Molecular Weight：

943.476

Exact Mass：

942.184143

Characteristics

PSA：

249.46000

XLogP3：

12.26450

Appearance：

colourless to light-yellow crystal

Density：

1.403 g/mL (20.84 °C)

Melting Point：

237 - 239 °C

Boiling Point：

750.7ºC at 760 mmHg

Flash Point：

68 °F

Refractive Index：

n20/D 1.5520(lit.)

Safety Information

hazard class code：

R43:May cause sensitization by skin contact. R51/53:Toxic to aquatic organisms, may cause long-term adverse effects in the aquatic environment .

safety instructions：

S24-S37-S61

Marks：

Xi,N

Lapatinib ditosylate monohydrate Use and Manufacturing

anticancer binds to a(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors atypical antipsychotic agent

Drug Function and Efficacy

Small molecule 4-anilinoquinazoline receptor tyrosine kinase inhibitor, inhibits epidermal growth factor receptor (ErbB1) and human epidermal growth factor receptor 2 (ErbB2). The half-inhibitory concentrations of breast cancer cell lines BT474 and SKBr3 sensitive to lapatinib are 25 and 32nmol/L, respectively, and enhances the efficacy of cisplatin on bladder cancer cell line RT112. It can inhibit epidermal growth factor-driven tumor growth in animal models and is effective against trastuzumab-resistant tumor cell lines.

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Lapatinib Tosylate Tablets
Ingredients	Lapatinib tosylate. Molecular weight: C29H26ClFN4O4S(C7H8O3S)2
Indication	In vitro, lapatinib tablets can inhibit CYP3A4 and CYP2C8 at therapeutic concentrations, and are mainly metabolized by CYP3A4. Drugs that inhibit the activity of this enzyme can significantly increase the blood concentration of lapatinib. Ketoconazole, 0.2g each time, twice a day, can increase the AUC of lapatinib by 3 to 7 times after 7 days, and extend the half-life by 1.7 times. Healthy volunteers took CYP3A4 inducers orally, 100 mg each time, twice a day, and changed to 200 mg each time after 3 days, twice a day for 17 days, and the AUC of lapatinib decreased by 72%. Lapatinib is a transporter of P-glycoprotein, and drugs that inhibit glycoproteins may increase the blood concentration of the drug.
Specifications	0.25g

Lapatinib Tosylate Tablets
Specifications	0.25 g

Lapatinib Tosylate Tablets
Ingredients	Lapatinib tosylate. Molecular weight: C29H26ClFN4O4S(C7H8O3S)2
Indication	In vitro, lapatinib tablets can inhibit CYP3A4 and CYP2C8 at therapeutic concentrations, and are mainly metabolized by CYP3A4. Drugs that inhibit the activity of this enzyme can significantly increase the blood concentration of lapatinib. Ketoconazole, 0.2g each time, twice a day, can increase the AUC of lapatinib by 3 to 7 times after 7 days, and extend the half-life by 1.7 times. Healthy volunteers took CYP3A4 inducers orally, 100 mg each time, twice a day, and changed to 200 mg each time after 3 days, twice a day for 17 days, and the AUC of lapatinib decreased by 72%. Lapatinib is a transporter of P-glycoprotein, and drugs that inhibit glycoproteins may increase the blood concentration of the drug.
Specifications	0.25g

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Registered Holders

MSN LABORATORIES PRIVATE LTD

United States
Active
HETERO LABS LTD

United States
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CHEMWERTH INC

United States
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Guide of Lapatinib ditosylate monohydrate

Description
Basic Attributes
Characteristics
Safety Information
Use and Manufacturing
Drug Function and Efficacy
Related Drugs
Registered Holders
Recommended Suppliers
Latest News
Learn More Other Chemicals

Lapatinib ditosylate monohydrate

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