Binding Mode
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Midostaurin

Binding Mode
Product Name
Midostaurin
CAS No.
120685-11-2
Chemical Name
Midostaurin
Synonyms
QTH113;CS-730;PKC412A;PKC 412A;PKC-412A;CGP 41231;Cgp 41251;Cgp-41251;Cgp 41 251;midostaruin
CBNumber
CB71315281
Molecular Formula
C35H30N4O4
Formula Weight
570.64
MOL File
120685-11-2.mol
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Midostaurin Property

Melting point:
235-260℃
Density 
1.47±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
Soluble in DMSO (15 mg/ml), MDC (10 mg/ml), methanol (5 mg/ml), 100% ethanol (2.5 mg/ml), and DMF (20 mg/ml).
form 
Tan solid
pka
14.19±0.70(Predicted)
color 
White
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
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Safety

Hazard Codes 
T
Risk Statements 
36/37/38
HS Code 
29329990
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P280Wear protective gloves/protective clothing/eye protection/face protection.

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

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
539648
Product name
Staurosporine, N-Benzoyl
Purity
A cell-permeable Staurosporine derivative that displays antitumor properties.
Packaging
1mg
Price
$289
Updated
2024/03/01
Alfa Aesar
Product number
J62917
Product name
Midostaurin
Packaging
1mg
Price
$119
Updated
2023/06/20
Alfa Aesar
Product number
J62917
Product name
Midostaurin
Packaging
5mg
Price
$424
Updated
2023/06/20
Cayman Chemical
Product number
10459
Product name
PKC 412
Purity
≥98%
Packaging
1mg
Price
$28
Updated
2024/03/01
Cayman Chemical
Product number
10459
Product name
PKC 412
Purity
≥98%
Packaging
5mg
Price
$84
Updated
2024/03/01
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Midostaurin Chemical Properties,Usage,Production

Binding Mode

The only available X-ray co-crystal structure of midostaurin is in complex with DYRK1A (dual specificity tyrosine phosphorylation regulated kinase 1A)(Fig.1). Midostaurin is anchored to the hinge with two hydrogen bonds: the lactam NH with amide carbonyl of Glu239; and the lactam carbonyl with amide NH of Leu241 (Fig.2).

Description

PKC-412 (120685-11-2) is a broad spectrum kinase inhibitor. Inhibited kinases include, but are not limited to; PKA, PKC, S6 Kinase, KDR, PKC, Akt, EGFR, VEGFR, PDGFR, c-kit, and FLT-3. Acute myeloid leukemia related mutant forms of FLT-3 are also inhibited both in vitro and in vivo. PKC-412 has been demonstrated to induce apoptosis and shows broad antiproliferative activity in various tumor cell lines. Cell Permeable

Uses

Midostaurin is used as a broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α, β, γ), PDFRβ, VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity. Due to this act which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors. Midostaurin was shown to possess antiproliferative characteristics via inhibition of protein kinase C, kinase insert domain receptor, and c-kit.

Definition

ChEBI: An organic heterooctacyclic compound that is the N-benzoyl derivative of staurosporine.

brand name

Rydapt

General Description

Class: receptor tyrosine kinase; Treatment: AML, SM; Other name: PKC-412, CGP41251; Elimination half-life = 20 h; Protein binding > 99%

Biological Activity

Broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms ( α , β , γ ), PDFR β , VEGFR2, Syk, PKCη, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.

target

Primary targets: FLT3, KIT

storage

Store at -20°C

References

1) Odgerel et al. (2008) The FLT3 inhibitor PKC412 exerts differential cell cycle effects on leukemic cells depending on the presence of FLT3 mutations; Oncogene, 27 3102 2) El Fitori et al. (2007) PKC 412 small-molecule tyrosine kinase inhibitor: single-compound therapy for pancreatic cancer; Cancer, 110 1457 3) Miyatake, et al. ( 2007) PKC412 (CGP41251) modulates the proliferation and lipopolysaccharide-induced inflammatory responses of RAW 264.macrophages; Biochem. Biophys. Res. Commun., 360 115 4) Bahlis et.al. (2005) N-Benzoylstaurosporine (PKC412) inhibits Akt kinase inducing apoptosis in multiple myeloma cells; Leuk. Lymphoma, 46 899 5) Fabbro et al., (2000) PKC-412 – a protein kinase inhibitor with a broad therapeutic potential; Anticancer Drug Des., 15 17

Midostaurin Preparation Products And Raw materials

Raw materials

Preparation Products

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Midostaurin Suppliers

Shanghai Zhibang Biological Medicine Co., LTD
Tel
021-54285032 18116461626
Fax
021-54285032
Email
25493162@qq.com
Country
China
ProdList
142
Advantage
58
Wuxi enqiao Pharmaceutical Technology Co., Ltd
Tel
0510-83591909 18018392058
Fax
0510-83591909
Email
info@enbridgepharm.com
Country
China
ProdList
237
Advantage
58
Fujian Kerui Pharmaceutical Co., Ltd.
Tel
+86-591-83309157; 18505919179
Fax
0591-83309157
Email
23115188@qq.com
Country
China
ProdList
18
Advantage
62
Wuhan Wiseman Bioengineering Co.,Ltd
Tel
027-59506022 13419526507
Fax
027-59506022
Email
13419526507@163.com
Country
China
ProdList
2990
Advantage
58
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
94657
Advantage
76
3B Pharmachem (Wuhan) International Co.,Ltd.
Tel
821-50328103-801 18930552037
Fax
86-21-50328109
Email
3bsc@sina.com
Country
China
ProdList
15839
Advantage
69
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Beijing HwrkChemical Technology Co., Ltd
Tel
010-89508211 18501085097
Fax
010-89508210
Email
sales.bj@hwrkchemical.com
Country
China
ProdList
8418
Advantage
55
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2123
Advantage
70
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19179
Advantage
64
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View Lastest Price from Midostaurin manufacturers

WUHAN FORTUNA CHEMICAL CO., LTD
Product
Midostaurin 120685-11-2
Price
US $0.00/KG
Min. Order
1KG
Purity
98%min
Supply Ability
30tons/month
Release date
2023-02-06
shandong perfect biotechnology co.ltd
Product
Midostaurin 120685-11-2
Price
US $0.00/g
Min. Order
1g
Purity
98% HPLC
Supply Ability
1kg
Release date
2023-08-01
Shaanxi Haibo Biotechnology Co., Ltd
Product
Midostaurin 120685-11-2
Price
US $0.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
2000ton
Release date
2023-09-08

120685-11-2, MidostaurinRelated Search:


  • CGP 41251MIDOSTAURIN(PKC412)
  • N-((5S,6R,7R,9R)-6-Methoxy-14-oxo-5,6,7,8,9,14,15,16-octahydro-17-oxa-4b,9a,15-triaza-5,9-Methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-MethylbenzaMide
  • PKC-412, CGP-41251
  • Midostaurin (PKC412)
  • PKC412 (Midostaurin)
  • CGP 41231
  • N-Benzoylstaurosporine
  • (Midostaurin) Benzoylstaurosporine
  • midostaruin
  • PKC412(Midostaurin,CGP41231,CGP41251)
  • PKC412 from Staurosporine
  • 4'-N-benzoylstaurosporine
  • Midostaurin, Benzoylstaurosporine, 4'-N-Benzoylstaurosporine, CGP 41251
  • Benzamide, N-((9S,10R,11R,13R)-2,3,9,10,11,12-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo(1,2,3-gh:3',2',1'-lm)pyrrolo(3,4-J)(1,7)benzodiazonin-11-yl)-N-methyl-
  • Benzamide, N-(2,3,9,10,11,12-hexahydro-9-methoxy-8-methyl-1-oxo-8,12-epoxy-1H,8H-2,7B,12A-triazadibenzo(A,G)cyclonona(cde)trinden-10-yl)-N-methyl-, (8alpha,9beta,10beta,12alpha)-
  • Benzoylstaurosporine
  • Cgp 41 251
  • Cgp 41251
  • Cgp-41251
  • Midostaurin
  • Midostaurin [inn]
  • [9S-(9α,10β,11β,13α)]-N-(2,3,10,11,12,13-Hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl)-N-methylbenzamide
  • PKC412 CGP 41231 CGP 41251 Midostaurin Benzoylstaurosporine
  • QTH113
  • Staurosporine, N-Benzoyl
  • MIDOSTAURIN; CGP-41251; PKC-412; PKC412;PKC 412
  • CS-730
  • MIDOSTAURIN (PKC412; CGP 41251)
  • Benzamide, N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-methoxy-9-methyl-1-oxo-9,13-epoxy-1H,9H-diindolo[1,2,3-gh:3',2',1'-lm]pyrrolo[3,4-j][1,7]benzodiazonin-11-yl]-N-methyl-
  • Midostaurin USP/EP/BP
  • Midaustorin
  • N-((5S,6R,7R,9S)-6-Methoxy-5-methyl-14-oxo-5,6,7,8,9,14,15,16-octahydro-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide
  • Midoridoline
  • N-((5S,6R,7R,9R)-6-Methoxy-5-methyl-14-oxo-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide
  • Midostaurin (Amorphous and Form II)
  • N-((5S,6R,7R,9R)-6-methoxy-5-methyl-14-oxo-5,6,7,8,9,14,15,16-octahydro-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-7-yl)-N-methylbenzamide
  • PKC 412A
  • PKC412A
  • PKC-412A
  • Midostaurin Impurity
  • 120685-11-2
  • 20685-11-2
  • C35H30N4O4
  • C325H30N4O4
  • antibiotic
  • Pharmaceutical