ChemicalBook > CAS DataBase List > TAS0728

TAS0728

Product Name
TAS0728
CAS No.
2088323-16-2
Chemical Name
TAS0728
Synonyms
AS0728;TAS0728;TPC-107;TAS0728, 10 mM in DMSO;TAS0728;TAS-0728;TAS 0728;TAS 0728,Inhibitor,EGFR,ErbB-1,inhibit,TAS0728,HER1,TAS-0728,Epidermal growth factor receptor;(R)-1-(1-Acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide;1H-Pyrazolo[3,4-d]pyrimidine-3-carboxamide, 4-amino-N-[4-[2-(dimethylamino)-2-oxoethyl]-2,3-dimethylphenyl]-1-[(3R)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-
CBNumber
CB55417169
Molecular Formula
C26H32N8O3
Formula Weight
504.58
MOL File
2088323-16-2.mol
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TAS0728 Property

Boiling point:
721.8±60.0 °C(Predicted)
Density 
1.35±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 125 mg/mL (247.73 mM; Need ultrasonic)
form 
A crystalline solid
pka
10.24±0.70(Predicted)
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0087131
Product name
TAS0728
Purity
99.53%
Packaging
10mg
Price
$550
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611316
Product name
TAS0728
Purity
>98%
Packaging
100mg
Price
$1802
Updated
2021/12/16
ChemScene
Product number
CS-0087131
Product name
TAS0728
Purity
99.53%
Packaging
100mg
Price
$2650
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611316
Product name
TAS0728
Purity
>98%
Packaging
250mg
Price
$3136.5
Updated
2021/12/16
Biorbyt Ltd
Product number
orb611316
Product name
TAS0728
Purity
>98%
Packaging
1g
Price
$5803.8
Updated
2021/12/16
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TAS0728 Chemical Properties,Usage,Production

Uses

TAS0728 is a potent, selective, orally active, irreversible and covalent-binding HER2 inhibitor, with an IC50 of 13 nM. TAS0728 also shows IC50s of 4.9, 8.5, 31, 65, 33, 25 and 86 nM for BMX、HER4、BLK、EGFR、JAK3、SLK and LOK respectively. Furthermore, TAS0728 exhibits robust and sustained inhibition of the phosphorylation of HER2, HER3, and downstream effectors[1].

in vivo

TAS0728 reveals the sustained and targeted inhibition of phosphorylation of HER2, HER3, AKT and ERK. TAS0728 also shows the ability of tumor regression and low toxicity[1].

Animal Model:Male nude mice
Dosage:7.5, 15, 30 and 60 mg/kg
Administration:Oral gavage; 7.5, 15, 30 and 60 mg/kg a day;14 days
Result:Rapidly eliminated within 24 hours.
Animal Model:Mice bearing NCI-N87 xenografts
Dosage:60 mg/kg
Administration:Oral gavage; 60 mg/kg a day; 14 days
Result:Revealed sustained target inhibition of HER2, HER3, AKT and ERK.
Animal Model:Mice with NCI-N87 HER2–amplified human gastric cancer
Dosage:7.5, 15, 30 and 60 mg/kg
Administration:Oral gavage; 7.5, 15, 30 and 60 mg/kg a day; 14 days
Result:Well tolerated in all mice.
Significant tumor regression was observed in mice treated with 60 mg/kg/day.
Animal Model:NCI-N87 peritoneal dissemination model
Dosage:30 and 60 mg/kg
Administration:Oral gavage; 30and 60 mg/kg a day; 120 days
Result:No evident toxicity, including diarrhea and body weight loss in the long-term dosing of TAS0728.

IC 50

HER4: 8.5 nM (IC50); HER2: 13 nM (IC50); EGFR: 65 nM (IC50); BMX: 4.9 nM (IC50); BLK: 31 nM (IC50); JAK3: 33 nM (IC50); SLK: 25 nM (IC50); LOK: 86 nM (IC50)

References

[1] Irie H, et al. TAS0728, A Covalent-binding, HER2-selective Kinase Inhibitor Shows Potent Antitumor Activity in Preclinical Models. Molecular cancer therapeutics. 2019;18(4):733-42. Epub 2019/02/23. DOI:10.1158/1535-7163.MCT-18-1085

TAS0728 Preparation Products And Raw materials

Raw materials

Preparation Products

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TAS0728 Suppliers

China 52 United States 6 Global 58
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3506
Advantage
58
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4757
Advantage
55
Lianyungang TengFa Biological Technology Co. Ltd
Tel
0518-85475186 18705131893
Fax
0518-85475186
Email
wang666xt@163.com
Country
China
ProdList
351
Advantage
55
Shanghai Beckham Medical Technology Co., Ltd
Tel
13816613772
Fax
QQ: 12922499
Email
huahero21@sina.com
Country
China
ProdList
2391
Advantage
55
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Fax
021-65675885
Email
info@efebio.com
Country
China
ProdList
9803
Advantage
58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Fan De(Beijing) Biotechnology Co., Ltd.
Tel
15911056312
Email
liming@bio-fount.com
Country
China
ProdList
9729
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32435
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

2088323-16-2, TAS0728Related Search:

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  • TAS0728
  • TAS0728;TAS-0728;TAS 0728
  • 1H-Pyrazolo[3,4-d]pyrimidine-3-carboxamide, 4-amino-N-[4-[2-(dimethylamino)-2-oxoethyl]-2,3-dimethylphenyl]-1-[(3R)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-
  • TAS 0728,Inhibitor,EGFR,ErbB-1,inhibit,TAS0728,HER1,TAS-0728,Epidermal growth factor receptor
  • (R)-1-(1-Acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide
  • TAS0728, 10 mM in DMSO
  • AS0728
  • TPC-107
  • 2088323-16-2
  • C26H32N8O3