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Postion:Product Catalog >API>Antineoplastic agents>Tinib Antineoplastic drugs> Imatinib
Imatinib
  • Imatinib
  • Imatinib

Imatinib NEW

Price $8 $6 $1
Package 1KG 25KG 100KG
Min. Order: 1KG
Supply Ability: g-kg-tons, free sample is available
Update Time: 2024-03-29

Product Details

Product Name: Imatinib CAS No.: 152459-95-5
Min. Order: 1KG Purity: 99%
Supply Ability: g-kg-tons, free sample is available Release date: 2024/03/29
Lead time: In stock, ready for shipment Packaging: bag/bottle/drum/IBC
Delivery: By express, by air, by sea Origin: Manufacturer, advantage product
CCOA, MSD: Available, contact us for details Name: Sun

 1. Materials information

Names

Nameimatinib
SynonymMore Synonyms

 Imatinib (STI571) Biological Activity

DescriptionImatinib is a tyrosine kinases inhibitor that inhibits c-Kit, Bcr-Abl, and PDGFR (IC50=100 nM) tyrosine kinases.
Related Catalog
Signaling Pathways >> Autophagy >> Autophagy
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Bcr-Abl
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Research Areas >> Cancer
Target

PDGFR:100 nM (IC50)

c-Kit:100 nM (IC50)

In VitroImatinib (STI571) inhibits c-Kit autophosphorylation, activation of MAPK, and activation of Akt without altering total protein levels of c-kit, MAPK, or Akt. The concentration that produces 50% inhibition for these effects is approximately 100 nM[1]. Imatinib (STI571) is very effective (in vitro IC50 of 25 nM) against the chronic myeloid leukemia-causing kinase Bcr-Abl. Imatinib also efficiently inhibits Kit (in vitro IC50, 410 nM) and PDGFR (in vitro IC50, 380 nM)[2]. Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and inhibits Bcr/Abl, v-Abl, Tel/Abl, the native PDGFβ receptor, and c-Kit, but it does not inhibit Src family kinases, c-Fms, Flt3, the EGFR or multiple other tyrosine kinases. Imatinib inhibits tyrosine phosphorylation and cell growth of Ba/F3 cells expressing Bcr/Abl, Tel/Abl, Tel/PDGFβR, and Tel/Arg with an IC50 of approximately 0.5 μM in each case, but it has no effect on untransformed Ba/F3 cells growing in IL-3 or on Ba/F3 cells transformed by Tel/JAK2[3]. The IC50s of Imatinib(STI571) is a multi-target inhibitor of v-Abl, c-Kit and on BON-1 and H727 cells after exposure for 48 h are 32.4 and 32.8 μM, respectively[4].
In VivoIn the phosphorothioate antisense oligodeoxynucleotides (PS-ASODN) group, tumor growth is inhibited by 59.437%, which is markedly higher than in the Imatinib (STI571) is a multi-target inhibitor of v-Abl, c-Kit and group (11.071%) and liposome negative control group (2.759%). Telomerase activity is significantly lower (P<0.01) in the PS-ASODN group (0.689±0.158) compare with the Imatinib group (1.838±0.241), liposome negative control group (2.013±0.273), and saline group (2.004±0.163)[5]. Imatinib (25 mg/kg/day, p.o.) suppresses the growth of endometriotic tissue and reduces the number of ovarian follicles in a rat model. Imatinib effectively treats experimental endometriosis by its inhibitor effects on angiogenesis and cell proliferation[6].
Cell AssayBON-1 cells (7,500 per well) and NCI-H727 cells (5,000 per well) are seeded into flat-bottomed 96-well plates in triplicate and allowed to adhere overnight in 10% fetal bovine serum-supplemented DMEM or RPMI 1640 complete medium, respectively; the medium is then exchanged for serum-free medium (negative control) or serum-free medium containing serial dilutions of Imatinib. After 48 h (control cultures do not reach confluence), the number of metabolically active cells is determined by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, and absorbance is measured in a Packard Spectra microplate reader at 540 nm. Growth inhibition is calculated. Experiments are done in triplicates[4].
Animal AdminMice[5] The 40 tumor-bearing SCID mice are randomly divided into four groups (10 mice per group): the PS-ASODN group (5 μM, each mouse receives 0.2 mL by intratumor injection once daily); Imatinib group (0.1 mg/g body weight); liposome negative control group (0.01 mL/g); and saline group (0.01 mL/g). The mice in each group receive the relevant treatment by intra-tumor injection once daily from day 7 to day 28 after implantation. After 28 d, the mice are sacrificed, and tumor weight and longest and shortest diameters are measured by electronic scale and vernier caliper, respectively. Inhibition of tumor growth is calculated. Rats[6] Adult female Wistar-Albino rats (220-240 g) are used. Twenty-one days after the first surgical procedure, the rats undergo a second laparotomy to evaluate the occurrence of endometriosis. Twenty-four rats have visually confirmed endometriotic implants and are randomized into three groups to receive Imatinib (25 mg/kg/day, p.o.), Anastrozole (0.004 mg/day, p.o.), or normal saline (0.1 mL, i.p.) for 14 days.
References

[1]. Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32.

[2]. Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9.

[3]. Okuda K, et al. ARG tyrosine kinase activity is inhibited by STI571.Blood. 2001 Apr 15;97(8):2440-8

[4]. Yao JC, et al. Clinical and in vitro studies of imatinib in advanced carcinoid tumors. Clin Cancer Res. 2007 Jan 1;13(1):234-40.

[5]. Sun XC, et al. Depletion of telomerase RNA inhibits growth of gastrointestinal tumors transplanted in mice. World J Gastroenterol. 2013 Apr 21;19(15):2340-7.

[6]. Yildiz C, et al. Effect of imatinib on growth of experimental endometriosis in rats. Eur J Obstet Gynecol Reprod Biol. 2016 Feb;197:159-63.

 Chemical & Physical Properties

Density1.3±0.1 g/cm3
Boiling Point451°C
Melting Point113°C
Molecular FormulaC29H31N7O
Molecular Weight493.603
Flash Point196°C
Exact Mass493.259003
PSA86.28000
LogP2.48
Vapour Pressure6.03E-24mmHg at 25°C
Index of Refraction1.672
Storage conditionRefrigerator

 Safety Information

Hazard CodesT,N
Risk PhrasesR23/24/25:Toxic by inhalation, in contact with skin and if swallowed . R40:Limited evidence of a carcinogenic effect. R48/23/24:Toxic: danger of serious damage to health by prolonged exposure through inhalation and in contact with skin . R51/53:Toxic to aq
Safety PhrasesS28-S36/37-S45-S61-S24/25-S23-S53
RIDADRUN 1662 6.1/PG 2
WGK Germany3
Packaging GroupII
Hazard Class6.1
HS Code2933990090

 Synthetic Route

Previous 1/13 Next
Article illustration

N-(5-Amino-2-me...

152460-10-1

Article illustration

4-(4-Methylpipe...

148077-69-4

~70%

Article illustration

Imatinib (STI57...

152459-95-5

Literature: CHEMAGIS LTD. Patent: EP1857454 A1, 2007 ; Location in patent: Page/Page column 4 ;
Article illustration

N-(5-Amino-2-me...

152460-10-1

Article illustration

Methyl 4-[(4-me...

314268-40-1

~90%

Article illustration

Imatinib (STI57...

152459-95-5

Literature: Shen, Xin; He, Xiao; Yang, Jidong; Wu, Shaohong; Zhan, Huaxing Patent: US2013/41149 A1, 2013 ; Location in patent: Paragraph 0025 ;
Article illustration

4-(4-methyl pip...

1044872-32-3

Article illustration

N-(5-Amino-2-me...

152460-10-1

~92%

Article illustration

Imatinib (STI57...

152459-95-5

Literature: Shen, Xin; He, Xiao; Yang, Jidong; Wu, Shaohong; Zhan, Huaxing Patent: US2013/41149 A1, 2013 ; Location in patent: Paragraph 0028 ;

 Precursor & DownStream

Precursor  7

Previous 1/2 Next

  • Article illustration CAS#:152460-10-1
    N-(5-Amino-2-me...

  • Article illustration CAS#:148077-69-4
    4-(4-Methylpipe...

  • Article illustration CAS#:314268-40-1
    Methyl 4-[(4-me...

  • Article illustration CAS#:1044872-32-3
    4-(4-methyl pip...

DownStream  2



  • Article illustration CAS#:571186-91-9
    Imatinib (Piper...

  • Article illustration CAS#:571186-93-1
    iMatinib relate...

 Customs

HS Code2933990090
Summary2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]- (9CI)
Imatinib
STI571
Imatinib (STI571)
Benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-N-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]-
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
4-[(4-methylpiperazin-1-yl)methyl]-N-(4-methyl-3-{[4-(pyridin-3-yl)pyrimidin-2-yl]amino}phenyl)benzamide
1iep
UNII-BKJ8M8G5HI
Benzamide, 4-((4-methyl)-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)-
MFCD05662257
4-[(4-Methyl-1-piperazinyl)methyl]-N-(4-methyl-3-{[4-(3-pyridinyl)-2-pyrimidinyl]amino}phenyl)benzamide
Imatinib free base
1xbb


 Names

Names-allyl-l-cysteine
SynonymMore Synonyms

 S-Allyl-L-cysteine Biological Activity

DescriptionS-Allyl-L-cysteine, one of the organosulfur compounds found in AGE, possess various biological effects including neurotrophic activity, anti-cancer activity, anti-inflammatory activity.
Related Catalog
Signaling Pathways >> Others >> Others
Research Areas >> Cancer
Research Areas >> Neurological Disease
Natural Products >> Others
Research Areas >> Inflammation/Immunology
Research Areas >> Metabolic Disease
Research Areas >> Others
In VitroIt is found that S-Allyl-L-cysteine could protect against amyloid-protein (A)-and tunicamycin-induced cell death in differentiated PC12 cells. Simultaneously applied S-Allyl-L-cysteine (1 μM) suppresses the cell death induced by Aβ25-35 and Aβ1-40 in a concentration-dependent manner, and neuronal integrity is almost completely retained. Simultaneously applied S-Allyl-L-cysteine significantly decreases the Aβ-induced level of ROS. The TEAC value of S-Allyl-L-cysteine is lower than that of oxidized GSH, and no antioxidant activity is observed. Intracellular GSH levels remains unaffected by treatment of neurons with S-Allyl-L-cysteine for 24 h. Furthermore, the increase in caspase-12 protein expression is suppressed by simultaneously adding 1 μM S-Allyl-L-cysteine [1]. S-Allyl-L-cysteine up to a concentration 1.0 mM does not exhibit any cytotoxic impact on morphology of myoblast and myotubes in culture observed under bright field microscope. TNF treatment leads to a significant decrease in the intracellular CK activity while S-Allyl-L-cysteine pre-treatment to TNF treated myotubes decreases the release of CK in media. S-Allyl-L-cysteine pre-treatment decreases the level of active form of this enzyme in S-Allyl-L-cysteine+TNF group. Similar observations are recorded at mRNA level for caspase-3. These results illustrate that S-Allyl-L-cysteine regulates apoptotic signals via suppressing the transcription and thus protein expression of caspase-3[2].
References

[1]. Kosuge Y, et al. S-allyl-L-cysteine selectively protects cultured rat hippocampal neurons from amyloid beta-protein- and tunicamycin-induced neuronal death. Neuroscience. 2003;122(4):885-95.

[2]. Dutt V, et al. S-allyl cysteine inhibits TNFα-induced skeletal muscle wasting through suppressing proteolysis and expression of inflammatory molecules. Biochim Biophys Acta. 2018 Apr;1862(4):895-906.

 Chemical & Physical Properties

Density1.191
Boiling Point300 ºC
Melting Point235-236 ºC
Molecular FormulaC6H11NO2S
Molecular Weight161.222
Flash Point135 ºC
Exact Mass161.051056
PSA88.62000
LogP1.31
Vapour Pressure0.0±1.3 mmHg at 25°C
Index of Refraction1.543
Storage condition2-8°C

 MSDS

S-Allyl-L-cysteine MSDS(Chinese)

 Safety Information

SymbolArticle illustration
GHS07
Signal WordWarning
Hazard StatementsH317
Precautionary StatementsP280
Hazard CodesF,C
Risk PhrasesR11:Highly Flammable. R22:Harmful if swallowed. R34:Causes burns. R20/21/22:Harmful by inhalation, in contact with skin and if swallowed .
Safety PhrasesS16-S26-S36/37/39-S45
RIDADRUN 2379 3/PG 2
WGK Germany3
RTECSEO4460000
Packaging GroupII
Hazard Class3.1
HS Code2930909090

 Synthetic Route

Previous 1/4 Next
Article illustration

N-Boc-S-allyl-L...

232953-12-7

~56%

Article illustration

S-Allyl-L-cyste...

21593-77-1

Literature: ISIS INNOVATION LIMITED Patent: US2012/178913 A1, 2012 ; Location in patent: Page/Page column 10-11 ;
Article illustration

L-Cysteine hydr...

52-89-1

Article illustration

allyl bromide

106-95-6

~70%

Article illustration

S-Allyl-L-cyste...

21593-77-1

Literature: Maldonado, Perla D.; Alvarez-Idaboy, J. Raul; Aguilar-Gonzalez, Adriana; Lira-Rocha, Alfonso; Jung-Cook, Helgi; Medina-Campos, Omar Noel; Pedraza-Chaverri, Jose; Galano, Annia Journal of Physical Chemistry B, 2011 , vol. 115, # 45 p. 13408 - 13417
Article illustration

L-cysteine

52-90-4

Article illustration

allyl bromide

106-95-6

~84%

Article illustration

S-Allyl-L-cyste...

21593-77-1

Literature: Koch; Keusgen, Michael Pharmazie, 1998 , vol. 53, # 10 p. 668 - 671

 Precursor & DownStream

Precursor  10

Previous 1/3 Next

  • Article illustration CAS#:232953-12-7
    N-Boc-S-allyl-L...

  • Article illustration CAS#:52-89-1
    L-Cysteine hydr...

  • Article illustration CAS#:106-95-6
    allyl bromide

  • Article illustration CAS#:52-90-4
    L-cysteine

DownStream  9

Previous 1/3 Next

  • Article illustration CAS#:2179-57-9
    Diallyl disulfide

  • Article illustration CAS#:539-86-6
    Allicin

  • Article illustration CAS#:127-17-3
    Pyruvic acid

  • Article illustration CAS#:52-90-4
    L-cysteine

 Customs

HS Code2930909090
Summary2930909090. other organo-sulphur compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%



2. Packaging of materials

  • For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.

  • For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product. 

                             Or smaller package 1kg/bottle, 10kgs/bottle as request. 


Article illustrationArticle illustration


3. Shipping & Delivery

  • By Express

Provide door to door service

Suitable for goods under 50kg

Delivery: 3-7 days

Cost: low cost

Article illustration


  • By Air

Provide airport to airport service

Suitable for goods over 50kg

Delivery: 3-14 days

Cost: high cost

Article illustration


  • By Sea

Provide seaport to seaport service

Suitable for goods over 100kg

Delivery: 2-45 days

Cost: low cost

Article illustration


4. Contact information

For more details, pls contact us freely.

Email address: Sun@fdachem.com

Mob: 86 13526505137

WhatsApp/Skype/Wechat/LINE: 86 13526505137











Company Profile Introduction

Henan Fengda Chemical Co., Ltd. is located in the High-tech Development Zone of Henan Province. Specializing in the production and sales of various fine chemical products required for industrial production, including chemical raw materials, organic raw materials, petrochemicals, chemical reagents, solvents, catalysts, and additives, etc.

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Henan Fengda Chemical Co., Ltd

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  • Since: 2023-02-10
  • Address: Room 01, 2288 E05, Building 14, East Henan University, Science and Technology Park, 279 Xisanhuan Ro
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