ChemicalBook > CAS DataBase List > Btk Kinase inhibitor

Btk Kinase inhibitor

Product Name
Btk Kinase inhibitor
CAS No.
1351636-18-4
Chemical Name
Btk Kinase inhibitor
Synonyms
ONO-BKT;ONO BTK;Tirabrutinib;TIRABRUTINIB;GS-4059;Btk Kinase inhibitor;ONO-4059(Tirabrutinib);Tirabrutinib free base;Isoleucine Impurity 18;Tirabrutinib (ONO-4059);ONO-4059;ONO 4059;ONO4059
CBNumber
CB02716154
Molecular Formula
C25H22N6O3
Formula Weight
454.48
MOL File
1351636-18-4.mol
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Btk Kinase inhibitor Property

Boiling point:
672.0±65.0 °C(Predicted)
Density 
1.412±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO:65.0(Max Conc. mg/mL);143.02(Max Conc. mM)
DMSO:PBS (pH 7.2) (1:2):0.3(Max Conc. mg/mL);0.66(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);66.01(Max Conc. mM)
Ethanol:1.0(Max Conc. mg/mL);2.2(Max Conc. mM)
form 
A crystalline solid
pka
3.16±0.20(Predicted)
color 
White to yellow
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

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

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

ChemScene
Product number
CS-5676
Product name
Tirabrutinib
Purity
99.31%
Packaging
5mg
Price
$50
Updated
2021/12/16
ChemScene
Product number
CS-5676
Product name
Tirabrutinib
Purity
99.31%
Packaging
10mg
Price
$90
Updated
2021/12/16
Activate Scientific
Product number
AS117581
Product name
ONO-4059
Purity
98+%
Packaging
1mg
Price
$94
Updated
2021/12/16
ChemScene
Product number
CS-5676
Product name
Tirabrutinib
Purity
99.31%
Packaging
50mg
Price
$250
Updated
2021/12/16
AK Scientific
Product number
2840DM
Product name
Tirabrutinib
Packaging
2mg
Price
$309
Updated
2021/12/16
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Btk Kinase inhibitor Chemical Properties,Usage,Production

Description

Btk Kinase inhibitor is highly potent and selective orally administered, small molecule, and also named tirabrutinib, Brutons tyrosine kinase (BTK) inhibitor being developed by Ono pharmaceutical and its licensee Gilead Sciences for the treatment of autoimmune disorders and haematological malignancies. 

brand name

VelexbruTM

Biological Functions

In March 2020, tirabrutinib was approved in  Japan to treat primary central nervous system lymphoma (PCNSL).  Tirabrutinib shows excellent selectivity against all kinases with cysteines in the ATP-binding site corresponding to Cys481 in BTK with the exception of BMX, TXK, and TEC? However, it displays weaker  BTK inhibition than ibrutinib (IC50 = 6.8 nM vs. 0.47  nM).

General Description

Class: non-receptor tyrosine kinase
Treatment: PCNSL
Elimination half-life = 6.5–8 h
Protein binding = 91%

Mechanism of action

The selective inhibition of cell growth by Btk Kinase inhibitor was due to blocking of BTK-mediated signaling through AKT and cellular protein kinase D. It can inhibit autophosphorylation of the BTK at the Tyr223 position through the ERK, AKT and PKD signaling pathways.

Side effects

Adverse effects of the Btk Kinase inhibitor that occurred in some patients were rash, vomiting, neutropenia, arthralgia, and malaise, and drug-related Grade 3–4 Adverse effects were neutropenia, leukopenia, anemia, hypophosphatemia, PT-INR increased, pneumonitis, and acute myeloid leukemia. in prior Japanese studies, rash, hematologic adverse effects, erythema multiforme, and constipation were frequent adverse effects in a Phase I/II study of some patients with PCNSL, and rash, hematologic adverse effects, and stomatitis were the most common adverse effects in a Phase II study of some patients with WM.

target

BTK

Btk Kinase inhibitor Preparation Products And Raw materials

Raw materials

Preparation Products

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Btk Kinase inhibitor Suppliers

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View Lastest Price from Btk Kinase inhibitor manufacturers

Hong Kong Tiansheng New Material Trading Co., Ltd
Product
ONO-4059 1351636-18-4
Price
US $3.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
10kg
Release date
2021-09-24
Hong Kong Tiansheng New Material Trading Co., Ltd
Product
ONO-4059 1351636-18-4
Price
US $3.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
100KG
Release date
2022-08-05
Qiuxian Baitai New Material Co., LTD
Product
Tirabrutinib 1351636-18-4
Price
US $1.20/g
Min. Order
1KG
Purity
99%
Supply Ability
500ton/Month
Release date
2021-11-08

1351636-18-4, Btk Kinase inhibitorRelated Search:

ONO-4059 (hydrochloride) Flumatinib Afatinib (BIBW 2992)

  • Btk Kinase inhibitor
  • ONO BTK
  • ONO-4059(GS-4059,Tirabrutinib) free base
  • ONO-BKT
  • 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one
  • Tirabrutinib (ONO-4059)
  • ONO-4059;ONO 4059;ONO4059
  • 6-amino-9-[(3R)-1-(but-2-ynoyl)pyrrolidin-3-yl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one
  • ONO-4059; ONO4059; ONO 4059; ONO-4059; GS 4059; GS-4059; GS4059; ONO-WG-307; TIRABRUTINIB
  • TIRABRUTINIB;GS-4059
  • Tirabrutinib
  • 8H-Purin-8-one, 6-amino-7,9-dihydro-9-[(3R)-1-(1-oxo-2-butyn-1-yl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-
  • ONO-4059(Tirabrutinib)
  • Tirabrutinib free base
  • ONO4059-Analog(BTK inhibitor)
  • Isoleucine Impurity 18
  • Tirabrutinib, 10 mM in DMSO
  • 1351636-18-4