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Sunitinib malate

Sunitinib malate structure

CAS No:
341031-54-7
Formula:
C22H27FN4O2.C4H6O5
Chemical Name:
Sunitinib malate
Synonyms:
Butanedioic acid,2-hydroxy-,(2S)-,compd. with N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (1:1);Butanedioic acid,hydroxy-,(2S)-,compd. with N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (1:1);1H-Pyrrole-3-carboxamide,N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-,(2S)-hydroxybutanedioate (1:1);Sunitinib malate;SU 011248;SU 11248;Sutent;Sunitinib L-malate;Sunitinib L-malate
Categories:
Active Pharmaceutical Ingredients > Antineoplastic Agents

Description

Sunitinib Malate (SU 11248 Malate) is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC50s of 80 nM and 2 nM, respectively.

Sunitinib malate Basic Attributes

Molecular Weight：

532.566

Exact Mass：

532.233337

EC Number：

1308068-626-2

HScode：

29337900

Characteristics

PSA：

172.06000

XLogP3：

2.77040

Density：

1.3600 g/mL at 25 °C(lit.)

Melting Point：

189-191°C

Boiling Point：

572.1ºC at 760mmHg

Flash Point：

163 °F

Refractive Index：

n20/D 1.455(lit.)

Water Solubility：

DMSO: >10mg/mL

Storage Conditions：

Store at +4°C

Safety Information

Transport codes：

NONH for all modes of transport

wgk germany：

hazard class code：

61-2-48/25-36/37-22-53

safety instructions：

53-22-36/37-24/25

Marks：

Precautionary statement(s)：

P201-P308 + P313

Hazard Statements：

H360-H372

Sunitinib malate Use and Manufacturing

A multi-kinase inhibitor targeting several receptor tyrosine kinases (RTK). Antineoplastic.

Drug Function and Efficacy

Sunitinib malate is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs), including platelet-derived growth factor receptors (PDGFRalpha; and PDGFRbeta;), vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor type 1 (CSF-1R), and glial cell line-derived neurotrophic factor receptor (RET). Biochemical and cellular assays have shown that it can inhibit the activity of these receptor tyrosine kinases (RTKs), and the inhibitory effect of sunitinib has been demonstrated in cell proliferation assays. The main metabolite has similar activity to sunitinib. In vivo results have shown that it can inhibit PDGFRbeta;- and VEGFR2-dependent tumor angiogenesis and inhibit the growth of tumor cells with dysregulated expression of the targeted receptor tyrosine kinases (PDGFR, RET, or KIT).

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

Sunitinib Malate Capsules
Ingredients	Chemical name of sunitinib malate: (Z)-N-[2-(diethylamino)ethyl-5-[(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-3-carbamoyl-1H-pyrrole malate.
Indication	CYP3A4 inhibitors: Strong CYP3A4 inhibitors, such as ketoconazole, can increase the plasma concentration of sunitinib. It is recommended to choose a concomitant medication that has no or minimal inhibitory effect on this type of enzyme. If it must be used simultaneously with a strong CYP3A4 inhibitor, it is necessary to consider reducing the dose of this product. Healthy volunteers taking a single dose of sunitinib malate and concurrently administered a strong CYP3A4 inhibitor (ketoconazole) can result in an increase of 49% and 51% in the total (sunitinib and its major active metabolite) Cmax and AUC0-infin; respectively. Sunitinib and strong inhibitors of the CYP3A4 enzyme system (for example: ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir,
Specifications	37.5mg

Sunitinib Malate Capsules
Ingredients	Chemical name of sunitinib malate: (Z)-N-[2-(diethylamino)ethyl-5-[(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-3-carbamoyl-1H-pyrrole malate.
Indication	CYP3A4 inhibitors: Strong CYP3A4 inhibitors, such as ketoconazole, can increase the plasma concentration of sunitinib. It is recommended to choose a concomitant medication that has no or minimal inhibitory effect on this type of enzyme. If it must be used simultaneously with a strong CYP3A4 inhibitor, it is necessary to consider reducing the dose of this product. Healthy volunteers taking a single dose of sunitinib malate and concurrently administered a strong CYP3A4 inhibitor (ketoconazole) can result in an increase of 49% and 51% in the total (sunitinib and its major active metabolite) Cmax and AUC0-infin; respectively. Sunitinib and strong inhibitors of the CYP3A4 enzyme system (for example: ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir,
Specifications	37.5mg

Sunitinib Malate Capsules
Ingredients	Chemical name of sunitinib malate: (Z)-N-[2-(diethylamino)ethyl-5-[(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-3-carbamoyl-1H-pyrrole malate.
Indication	CYP3A4 inhibitors: Strong CYP3A4 inhibitors, such as ketoconazole, can increase the plasma concentration of sunitinib. It is recommended to choose a concomitant medication that has no or minimal inhibitory effect on this type of enzyme. If it must be used simultaneously with a strong CYP3A4 inhibitor, it is necessary to consider reducing the dose of this product. Healthy volunteers taking a single dose of sunitinib malate and concurrently administered a strong CYP3A4 inhibitor (ketoconazole) can result in an increase of 49% and 51% in the total (sunitinib and its major active metabolite) Cmax and AUC0-infin; respectively. Sunitinib and strong inhibitors of the CYP3A4 enzyme system (for example: ketoconazole, itraconazole, clarithromycin, atazanavir, indinavir, nefazodone, nelfinavir, ritonavir,
Specifications	25mg

See More Related Drugs

Registered Holders

CDYMAX (INDIA) PHARMA PRIVATE LTD

United States
Active
HIKMA PHARMACEUTICALS LLC

United States
Active
RELIANCE LIFE SCIENCES PVT LTD

United States
Active

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