804551-71-1

Basic information

• Product Name: CHIR-258
• Synonyms: CHIR-258(TKI-258, Dovitinib)
• CAS NO: 804551-71-1
• Molecular Formula: C21H21FN6O
• Molecular Weight: 392.4294432
• Mol File: 804551-71-1.mol

Chemical Properties

• Appearance: /
• CAS DataBase Reference: CHIR-258(CAS DataBase Reference)
• NIST Chemistry Reference: CHIR-258(804551-71-1)
• EPA Substance Registry System: CHIR-258(804551-71-1)

Safety Data

• Hazardous Substances Data: 804551-71-1(Hazardous Substances Data)

Usage

Uses

Used in Biological Research:
CHIR-258 is used as a research tool for studying the role of specific protein kinases in cellular processes, aiding in the understanding of their functions and potential as therapeutic targets.
Used in Pharmaceutical Development:
CHIR-258 is used as a potential therapeutic agent for the treatment of diseases such as cancer and inflammatory disorders, due to its selective inhibition of protein kinases like Lck, Lck-SH2, and Lck-SH3.
Used in Cancer Treatment:
In the field of oncology, CHIR-258 is used as a targeted therapy to inhibit the activity of specific protein kinases that are implicated in the development and progression of cancer.
Used in Inflammatory Disorders:
CHIR-258 is used as a potential treatment for inflammatory disorders, leveraging its ability to inhibit protein kinases that play a role in inflammation pathways.
Further research is necessary to fully explore the therapeutic and diagnostic potential of CHIR-258 in various applications.

InChI:InChI=1/C21H21FN6O.C3H6O3.H2O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29;1-2(4)3(5)6;/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29);2,4H,1H3,(H,5,6);1H2

Upstream product

• 402948-37-2 [6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]acetic acid ethyl ester 
• 77326-36-4 2-amino-6-fluorobenzonitrile 
• 1635-61-6 5-chloro-2-nitroaniline 
• 54998-08-2 4-(4-methylpiperazino)-1,2-diaminobenzene 
• 23491-48-7 5-(4-methylpiperazine-1-yl)-2-nitroaniline 
• 109-01-3 1-methyl-piperazine 

Relevant articles and documents

Method for preparing dovitinib intermediate with microchannel reaction device

The invention discloses a method for preparing a dovitinib intermediate with a microchannel reaction device. The method comprises the following steps: (1) dissolving hydrochloric acid in ethanol to form a mixed solution, and enabling the mixed solution an

Preparation method of dovitinib

The invention relates to a drug preparation method, in particular to a preparation method of dovitinib. A final product 4-amino-5-fluoro-3-(5-(4-methylpiperazine-1-yl)-1H- benzo[d]imidazol-2-yl) quinolone-2-(1H)-one is prepared by reacting ethyl 2-(5)-(4-methylpiperazine-1-yl)-1H-benzo[d]imidazol-2-yl) acetate with 2-amino-6-fluorobenzonitrile. The method is simple, convenient, high in safety and particularly suable for industrial production, the product yield and purity are high, and reaction conditions are mild.

TREATMENT OF MELANOMA

Methods of treating melanoma include administering a compound of Structure (I), a tautomer of the compound, a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable salt or the tautomer, or a mixture thereof to a subject. The comp

Formulation of Quinolinones

A pharmaceutical formulation, comprising: a compound of formula (I), a tautomer of the compound, a salt of the compound, a salt of the tautomer, or a mixture thereof and at least one ingredient selected from the group consisting of (i) cellulose; (ii) sil

LHMDS mediated tandem acylation-cyclization of 2-aminobenzenecarbonitriles with 2-benzymidazol-2-yl acetates: A short and efficient route to the synthesis of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones

We herein describe the discovery of a mild, one-pot tandem acylation-cyclization for the synthesis of 4-amino-3-benzimidazol-2- ylhydroquinolin-2-ones from 2-aminobenzenecarbonitriles and ethyl 2-benzimidazol-2-yl acetates.

The chemical development of CHIR-258

This paper is a case history of the early stage chemical development of CHIR-258 (4-amino-5-fluoro-3-[6-(4-methyl-1-piperazinyl)-1H-benzimidazol-2-yl]- 2(1H)-quinolinone, DL-lactate salt), a vascular endothelial growth factor (VEGF) kinase inhibitor for t

METHODS FOR TREATING DRUG RESISTANT CANCER

A method for treating drug-resistant cancer, includes: administering to a patient in need thereof, a compound of formula I, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comp

TREATMENT OF METASTASIZED TUMORS

Methods of treating metastatic cancer such as metastasized tumors include administering a compound of Structure I, a tautomer of the compound, a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable salt or the tautomer, or a mix

METHODS FOR SYNTHESIZING HETEROCYCLIC COMPOUNDS

A method for synthesizing a heterocyclic compound includes: reacting 1-methylpiperazine with 5-chloro-2-nitroaniline at an internal temperature sufficient to provide a compound of Formula VIH The 1-methylpiperazine and the 5-chloro-2-nitroaniline are reac

CRYSTALLINE AND OTHER FORMS OF 4-AMINO-5-FLUORO-3-[6-(4-METHYLPIPERAZIN-1-YL)-1H-BENZIMIDAZOL-2-YL]-1H-QUINOLIN-2-ONE LACTIC ACID SALTS

The present invention relates to non-hydrate crystalline forms of 4-amino- 5-fluoro-3 -[6-(4-methylpiperazin- 1 -yl)- 1 H-benzimidazol-2-yl] - 1 H-quinolin-2-one lactic acid salts, solid pharmaceutical formulations containing the same and methods of use. The present invention also relates to crystalline hydrates of 4-arnino-5-fiuoro-3-[6-(4- methylpiperazin-l-yl)-lH-benzimidazol-2-yl]-lH-quinolin-2-one lactic acid salts, pharmaceutical formulations containing the same and methods of use related thereto. The present invention further relates to crystalline solvates of 4-amino-5-fluoro-3-[6-(4- methylpiperazin-l-yl)-lH-benzimidazol-2-yl]-lH-quinolin-2-one lactic acid salts.