Binding Mode
ChemicalBook > CAS DataBase List > Midostaurin

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
More
Less

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.
More
Less

Safety

Hazard Codes 
T
Risk Statements 
36/37/38
HS Code 
29329990
More
Less

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..…

More
Less

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
More
Less

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

More
Less

Midostaurin Suppliers

Canada 1 China 196 China Hong Kong 1 India 11 Israel 1 Italy 1 United Kingdom 4 United States 17 Global 232
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2123
Advantage
70
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32165
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
Country
United States
ProdList
19553
Advantage
58
TargetMol Chemicals Inc.
Tel
Email
support@targetmol.com
Country
United States
ProdList
38632
Advantage
58
ApexBio Technology
Tel
--
Fax
--
Email
sales@apexbt.com
Country
United States
ProdList
6251
Advantage
58
BOC Sciences
Tel
16314854226
Email
info@bocsci.com
Country
United States
ProdList
9923
Advantage
65
Focus Biomolecules
Tel
--
Fax
--
Email
sales@focusbiomolecules.com
Country
United States
ProdList
1284
Advantage
58
Cayman Chemical Company
Tel
--
Fax
--
Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81
LC Laboratories
Tel
--
Fax
--
Email
custserv@lclabs.com
Country
United States
ProdList
503
Advantage
50
Creative Enzymes
Tel
--
Fax
--
Email
info@creative-enzymes.com
Country
United States
ProdList
6057
Advantage
58
MedChemExpress
Tel
--
Fax
--
Email
sales@medchemexpress.com
Country
United States
ProdList
6398
Advantage
58
Riedel-de Haen AG
Tel
--
Fax
--
Country
United States
ProdList
6773
Advantage
87
LKT Laboratories, Inc.
Tel
--
Fax
--
Email
info@lktlabs.com
Country
United States
ProdList
2164
Advantage
64
Santa Cruz Biotechnology, Inc.
Tel
--
Fax
--
Email
scbt@scbt.com
Country
United States
ProdList
3597
Advantage
60
More
Less

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:

CYCLOPAMINE Cantharidin Troglitazone ZM 447439 CGP52421 Benzamide, N-[(9S,10R,11R,13R)-2,3,10,11,12,13-hexahydro-10-hydroxy-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- 3 Hydroxy Midostaurin Epimer 2 (CGP52421 Epimer 2) 3 Hydroxy Midostaurin Epimer 1 (CGP52421 Epimer 1) Epothilone D Ibrutinib CARBAZOL-9-YL-METHANOL 9-ISOPROPYLCARBAZOLE 11,12-Dihydroindolo[2,3-a]carbazole Midostaurin K-252C

  • 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