Midostaurin

ChemicalBook > CAS DataBase List > 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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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