ChemicalBook >> CAS DataBase List >>Midostaurin

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
Molecular Weight:
570.64
MDL Number:
MFCD10687105
MOL File:
120685-11-2.mol
Last updated:2024-11-19 15:53:33

Midostaurin Properties

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).
pka 14.19±0.70(Predicted)
form Tan solid
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.
FDA UNII ID912S5VON
NCI Dictionary of Cancer Terms midostaurin; N-benzoyl-staurosporine
NCI Drug Dictionary midostaurin
ATC code L01EX10

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS08
Signal word  Danger
Hazard statements  H360FD
Precautionary statements  P201-P202-P280-P308+P313-P405-P501
Hazard Codes  T
Risk Statements  36/37/38
HS Code  29329990
NFPA 704
0
2 0

Midostaurin price More Price(40)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich 539648 Staurosporine, N-Benzoyl A cell-permeable Staurosporine derivative that displays antitumor properties. 120685-11-2 1mg $289 2024-03-01 Buy
Alfa Aesar J62917 Midostaurin 120685-11-2 1mg $119 2023-06-20 Buy
Alfa Aesar J62917 Midostaurin 120685-11-2 5mg $424 2023-06-20 Buy
Cayman Chemical 10459 PKC 412 ≥98% 120685-11-2 1mg $28 2024-03-01 Buy
Cayman Chemical 10459 PKC 412 ≥98% 120685-11-2 5mg $84 2024-03-01 Buy
Product number Packaging Price Buy
539648 1mg $289 Buy
J62917 1mg $119 Buy
J62917 5mg $424 Buy
10459 1mg $28 Buy
10459 5mg $84 Buy

Midostaurin Chemical Properties,Uses,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).
Figure 1. Co-crystal structure of midostaurin in  complex with human DYRK1A (PDB ID: 4NCT).Figure 2. Summary of midostaurin–human DYRK1A interactions based on their co-crystal structure.

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

Global( 232)Suppliers
Supplier Tel Email Country ProdList Advantage
shandong perfect biotechnology co.ltd
+86-53169958659 +86-13153181156 sales@sdperfect.com China 294 58
Hangzhou ICH Biofarm Co., Ltd
+86-0571-28186870; +undefined8613073685410 sales@ichemie.com China 998 58
Shaanxi Haibo Biotechnology Co., Ltd
+undefined18602966907 qinhe02@xaltbio.com China 997 58
Hangzhou FandaChem Co.,Ltd.
+8615858145714 FandaChem@Gmail.com China 9214 55
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32957 60
career henan chemical co
+86-0371-86658258 +8613203830695 sales@coreychem.com China 29884 58
Biochempartner
0086-13720134139 candy@biochempartner.com CHINA 965 58
BOC Sciences
+1-631-485-4226 inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd
+86-023-6139-8061 +86-86-13650506873 sales@chemdad.com China 39894 58
TopScience Biochemical
00852-68527855 info@itopbiochem.com China Hong Kong 902 58

View Lastest Price from Midostaurin manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Midostaurin pictures 2024-11-22 Midostaurin
120685-11-2
US $0.00 / KG 1KG 98%min 30tons/month WUHAN FORTUNA CHEMICAL CO., LTD
Midostaurin pictures 2024-11-19 Midostaurin
120685-11-2
US $0.00 / g 1g 98% HPLC 1kg shandong perfect biotechnology co.ltd
Midostaurin pictures 2024-11-18 Midostaurin
120685-11-2
US $47.00-128.00 / mg 99.56% 10g TargetMol Chemicals Inc.
  • Midostaurin pictures
  • Midostaurin
    120685-11-2
  • US $0.00 / KG
  • 98%min
  • WUHAN FORTUNA CHEMICAL CO., LTD
  • Midostaurin pictures
  • Midostaurin
    120685-11-2
  • US $0.00 / g
  • 98% HPLC
  • shandong perfect biotechnology co.ltd
  • Midostaurin pictures
  • Midostaurin
    120685-11-2
  • US $47.00-128.00 / mg
  • 99.56%
  • TargetMol Chemicals Inc.

Midostaurin Spectrum

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 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 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 PKC412(Midostaurin,CGP41231,CGP41251) PKC412 from Staurosporine QTH113 Staurosporine, N-Benzoyl MIDOSTAURIN; CGP-41251; PKC-412; PKC412;PKC 412 CS-730 MIDOSTAURIN (PKC412; CGP 41251) 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