Anticancer drug Uses
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Sunitinib Malate

Anticancer drug Uses
Product Name
Sunitinib Malate
CAS No.
341031-54-7
Chemical Name
Sunitinib Malate
Synonyms
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 (2S)-hydroxybutanedioate;Sunitinib L-malate;(Z)-N-(2-(Diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrr;CS-308;NSC2677;SU112248;NSC 2677;NSC-2677;SU 011248;Sunitinib MaL
CBNumber
CB22131216
Molecular Formula
C26H33FN4O7
Formula Weight
532.57
MOL File
341031-54-7.mol
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Sunitinib Malate Property

Melting point:
189-191°C
storage temp. 
room temp
solubility 
DMSO: >10mg/mL
form 
powder
color 
Orange
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
InChI
InChI=1/C22H27FN4O2.C4H6O5/c1-5-27(6-2)10-9-24-22(29)20-13(3)19(25-14(20)4)12-17-16-11-15(23)7-8-18(16)26-21(17)28;5-2(4(8)9)1-3(6)7/h7-8,11-12,25H,5-6,9-10H2,1-4H3,(H,24,29)(H,26,28);2,5H,1H2,(H,6,7)(H,8,9)/b17-12-;/t;2-/s3
InChIKey
XGQXULJHBWKUJY-LYIKAWCPSA-N
SMILES
[C@@H](O)(C(=O)O)CC(=O)O.C(/C1NC(C)=C(C(=O)NCCN(CC)CC)C=1C)=C1/C(NC2=CC=C(F)C=C/12)=O |&1:0,r|
CAS DataBase Reference
341031-54-7(CAS DataBase Reference)
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Safety

Hazard Codes 
T
Risk Statements 
61-2-48/25-36/37-22-53
Safety Statements 
53-22-36/37-24/25
WGK Germany 
2
HS Code 
29337900
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H360May damage fertility or the unborn child

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P308+P313IF exposed or concerned: Get medical advice/attention.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PZ0012
Product name
Sunitinib malate
Purity
≥98% (HPLC)
Packaging
5mg
Price
$146
Updated
2024/03/01
Sigma-Aldrich
Product number
PZ0012
Product name
Sunitinib malate
Purity
≥98% (HPLC)
Packaging
25mg
Price
$570
Updated
2024/03/01
Cayman Chemical
Product number
13159
Product name
Sunitinib Malate
Purity
≥98%
Packaging
1mg
Price
$30
Updated
2024/03/01
Cayman Chemical
Product number
13159
Product name
Sunitinib Malate
Purity
≥98%
Packaging
5mg
Price
$60
Updated
2024/03/01
Cayman Chemical
Product number
13159
Product name
Sunitinib Malate
Purity
≥98%
Packaging
10mg
Price
$105
Updated
2024/03/01
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Sunitinib Malate Chemical Properties,Usage,Production

Anticancer drug

Sunitinib malate is a kind of novel oral multi-targeted anticancer drugs and belongs to multi-targeted tyrosine kinase inhibitor with its trade name being “suntent”. It was successfully developed by Pfizer Company and has dual anti-tumor effect. Moreover, it is the only therapeutic drug which can go beyond the 2-year survival period of advanced kidney cancer and plays a central role in the field of carcinoma and gastrointestinal stromal tumor therapeutic areas. It entered into market in February 2006 in the United States. This drug was the first anti-cancer drug which was approved by the US FDA and can simultaneously treat two diseases.
Sunitinib exerts its therapeutic role through preventing the tumor cells from getting the blood and nutrients needed for growth. Clinical trials have showed that the drug can delay the growth rate of gastrointestinal stromal tumors, and can shrink the size of renal cell tumors. Sunitinib malate is the first novel targeted drug being capable of selectively targets drugs for a variety of new tyrosine kinase receptors. It combine two kinds of anti-tumor mechanisms including both stopping the formation of anti-angiogenic which is responsible for supplying blood to tumor and direct attack of tumor cells. It represents the advent of a new round of targeted therapies, being able to attack the tumor directly without the toxicity of the conventional chemotherapy.
The indications of Sunitinib malate are as follows:
1, Patients who failed in the treatment with matinib mesylate or of intolerant gastrointestinal stromal tumors (GIST).
2, inoperable advanced renal cell carcinoma (RCC).
3, advanced pancreatic endocrine tumors.
The above information is edited by the Chemicalbook of Dai Xiongfeng.

Uses

Anti-cancer drugs

Description

Sunitinib is a small molecule inhibitor of receptor tyrosine kinases, including FLK1 (Ki = 9 nM), PDGFRβ (Ki = 8 nM), and FLT3. It is at least 10-fold selective for FLK1 and PDGFRβ over a variety of tyrosine kinases in a panel, including EGFR, Cdk2, Met, IGFR-1, Abl, and Src. Sunitinib inhibits VEGF-dependent FLK1 and PDGF-dependent PDGFRβ phosphorylation (IC50s = 10 and 10 nM, respectively) as well as phosphorylation of FLT3 and FLT3 carrying the activating internal tandem duplication mutation (FLT3-ITD; IC50s = 250 and 50 nM, respectively). It decreases VEGF- and FGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC50s = 30 and 700 nM, respectively) and reduces tumor growth in a variety of mouse xenograft models when administered at doses ranging from 20 to 80 mg/kg per day. Formulations containing sunitinib have been used in the treatment of gastrointestinal stromal tumors and metastatic renal cell carcinoma.

Chemical Properties

Yellow Solid

Uses

Sunitinib Malate (Sutent, SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit.

Uses

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit

Uses

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

brand name

(Pfizer).

General Description

Sunitinib is available in 12.5-, 25-, and 50-mg capsules fororal administration for the treatment of advanced RCC andGIST upon the failure of imatinib. The agent is a multikinaseinhibitor and has been shown to inhibit PDGF-R,VEGF-R, Kit, RET, and the colony-stimulating factor receptor(CSR-1R). The result of this spectrum of activity isa slowing of tumor progression and inhibition of angiogenesisboth of which are useful in the highly vascularizedcancers, RCC and GIST. The median TTP (time to tumorprogression) was 27.3 weeks for sunitinib and 6.4 weeks with a median time of 24.1 weeks for sunitinib and 6 weeksfor placebo. The agent is well absorbed upon oral administration,and both the parent and major metabolite are highly(90%–95%) protein bound. Metabolism is mediated primarilyby CYP3A4 to give the N-desethyl derivative, which isthe major metabolite (23%–37%), equally active with theparent and undergoes further metabolism by CYP3A4. Theterminal elimination half-life for the parent and N-desethylderivative are 40 to 60 hours and 80 to 110 hours, respectively.Elimination occurs primarily via the feces. Commonadverse effects of sunitinib include fatigue, diarrhea, yellowskin discoloration, anorexia, nausea, and mucositis.Mild myelosuppression has been reported in patients withGIST including neutropenia, lymphopenia, thrombocytopenia,and anemia. There have been reports of cardiotoxicityincluding decreases in left ventricular ejectionfraction, which occurred in 11% of patients during a GISTstudy.

Biological Activity

Potent, ATP-competitive VEGFR, PDGFR β and KIT inhibitor (K i values are 2, 9, 17, 8 and 4 nM for VEGFR -1, -2, -3, PDGFR β and KIT respectively). Also inhibits cellular receptor phosphorylation of FLT3, RET and CSF-1R. Exhibits antiangiogenic and antitumor activity in multiple xenograft models.

Biochem/physiol Actions

Sunitinib has greater bioavailability and potency compared to other inhibitors. It prevents angiogenesis.

storage

Store at +4°C

References

1) Deeks et al. (2006), Sunitinib; Drugs, 66 2255 2) Guo et al. (2006), Inhibition of phosphorylation of the colony-stimulating factor-1 receptor (c-Fms) tyrosine kinase in transfected cells by ABT-869 and other tyrosine kinase inhibitors; Mol. Cancer. Ther., 5 1007 3) O’Farrell et al. (2003), SU11248 is a novel FLT3 yrosine kinase with potent activity in vitro and in vivo; Blood, 101 3597 4) Roskoski et al. (2007), Sunitinib: a EGF and PDGF receptor protein kinase and angiogenesis inhibitor; Biochem. Biophys. Res. Commun., 356 323

Sunitinib Malate Preparation Products And Raw materials

Raw materials

Preparation Products

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Sunitinib Malate Suppliers

Canada 3 China 367 China Hong Kong 1 Czech Republic 2 Germany 1 India 39 Israel 2 Poland 1 South Korea 1 Spain 2 The Netherlands 1 United Kingdom 7 United States 35 Global 462
Triveni chemicals
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View Lastest Price from Sunitinib Malate manufacturers

Sinoway Industrial co., ltd.
Product
Sunitinib Malate 341031-54-7
Price
US $0.00-0.00/Kg/Bag
Min. Order
1Kg/Bag
Purity
0.99
Supply Ability
20 tons
Release date
2024-06-27
HEBEI SHENGSUAN CHEMICAL INDUSTRY CO.,LTD
Product
Sunitinib Malate 341031-54-7
Price
US $100.00-75.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
5000
Release date
2024-08-22
WUHAN FORTUNA CHEMICAL CO., LTD
Product
Sunitinib Malate 341031-54-7
Price
US $0.00/Kg/Bag
Min. Order
1KG
Purity
99%min
Supply Ability
10kg
Release date
2021-09-23

341031-54-7, Sunitinib MalateRelated Search:

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  • EZSolution Sunitinib Malate
  • Malic acid Shu
  • 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 (2S)-2-hydroxybutanedioic acid (1:1) salt
  • SU 011248
  • SU112248
  • Sunitinib Malate(SU 11248)
  • Butanedioic acid, 2
  • N-(2-(Diethylamino)ethyl)-5-((Z)-(5-fluoro-1
  • (Z)-N-(2-(Diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrr
  • SUNITINIB MALATE
  • 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 (2S)-hydroxybutanedioate
  • CS-308
  • SUNITINIB MALATE (SU 11248 MALATE)
  • SU-11248;SU11248;SUTENT; SUNITINIB
  • Sunitinib Malate(Sutent)
  • 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)
  • N-(2-(DiethylaMino)ethyl)-5-((Z)-(5-fluoro-1,2-dih
  • SU11248; SUTENT
  • 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
  • (Z)-N-(2-(diethylaMino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)Methyl)-2,4-diMethyl-1H-pyrrole-3-carboxaMide (S)-2-hydroxysuccinate
  • N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide(2S)-2-hydroxybutanedioatesalt
  • (Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide ,(S)-2-hydroxysuccinic acid
  • Sunitinib malate 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 (2S)-hydroxybutanedioate
  • Sunitinib (SU 11248) Malate
  • Sunitinib Mablate
  • Sunitinib L-malate
  • SU 11248 (Malate)
  • Sunitinib MaL
  • Sunitinib Malate USP/EP/BP
  • Sunitinib Malate DISCONTINUED
  • Sunitanib Maleate
  • Sunitinib Malate API
  • Sunitinib MalateQ: What is Sunitinib Malate Q: What is the CAS Number of Sunitinib Malate Q: What is the storage condition of Sunitinib Malate Q: What are the applications of Sunitinib Malate
  • Sunitinib API
  • NSC 2677
  • NSC2677
  • NSC-2677
  • Sunitinib Maleat
  • Sunitinib Malate (Sunitinib L-Malate)
  • Sunitinib CRS
  • Sutent|||SU 11248 (Malate)|||SU 11248|||Sunitinib
  • 341031-54-7
  • 341013-54-7
  • C28H38N4O7
  • C22H27FN4O2C4H2O5
  • APIs
  • Inhibitors
  • Oxetanes
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pfizer compounds
  • Pharmaceuticals
  • Tyrosine Kinase Inhibitors
  • SU-11248
  • 341031-54-7