TAS6417

Product Name: TAS6417
CAS No.: 1661854-97-2
Chemical Name: TAS6417
Synonyms: CLN-081;TAS6417;Zipalertinib;TAS6417 TAS-6417;TAS6417/Zipalertinib;TAS6417, 10 mM in DMSO;Zipalertinib (TAS-6417);TAS-6417;TAS 6417;TAS6417;(S)-N-[4-Amino-6-methyl-5-(3-quinolyl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl]acrylamide;2-Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizi
CBNumber: CB64796695
Molecular Formula: C23H20N6O
Formula Weight: 396.44
MOL File: 1661854-97-2.mol

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TAS6417 Property

Boiling point:: 756.6±60.0 °C(Predicted)
Density: 1.40±0.1 g/cm3(Predicted)
storage temp.: 4°C, protect from light, stored under nitrogen
solubility: DMSO:20.0(Max Conc. mg/mL);50.44(Max Conc. mM)
form: Solid
pka: 12.81±0.40(Predicted)
color: White to yellow
InChIKey: MKCYPWYURWOKST-INIZCTEOSA-N
SMILES: C(N[C@H]1C=C(C)C2N(C1)C1=NC=NC(N)=C1C=2C1=CC2C(N=C1)=CC=CC=2)(=O)C=C

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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.

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.

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

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N-Bromosuccinimide Price

AK Scientific

Product number: 2080EF
Product name: CID117918742
Packaging: 1mg
Price: $387
Updated: 2021/12/16

Biosynth Carbosynth

Product number: FT166464
Product name: TAS 6417
Packaging: 2mg
Price: $400
Updated: 2021/12/16

ChemScene

Product number: CS-0044757
Product name: TAS6417
Purity: 99.55%
Packaging: 5mg
Price: $450
Updated: 2021/12/16

AK Scientific

Product number: 2080EF
Product name: CID117918742
Packaging: 2mg
Price: $590
Updated: 2021/12/16

ChemScene

Product number: CS-0044757
Product name: TAS6417
Purity: 99.55%
Packaging: 10mg
Price: $750
Updated: 2021/12/16

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TAS6417 Chemical Properties,Usage,Production

Uses

Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM[1][2].

in vivo

Zipalertinib (TAS6417) (10-200 mg/kg) causes persistent tumor regression in vivo in EGFR exon 20 insertion-driven tumor models. TAS6417 inhibits mutant EGFR in tumors but not WT EGFR in skin tissues^[1].
Zipalertinib (TAS6417) had no effect on EGFR-independent proliferation in NCI-H23 or NCI-H460 cells^[1].
Zipalertinib (TAS6417) administered at 20 mg/kg, which achieves complete suppression of tumor growth, induces a significant decrease in pEGFR, leading to reduction of pAKT and pERK at 1 h. The inhibitory effect is still noted at 6 h, and phosphorylation of EGFR, ATK, and ERK recovered by 24 h^[1].
Zipalertinib (TAS6417) (100 and 200 mg/kg/day) prolongs survival of animals bearing lung cancer^[1].

Animal Model:	Mice implanted with NCI-H1975 EGFR D770_N771insSVD xenografts^[1].
Dosage:	50 and 100 mg/kg.
Administration:	Orally once daily for 14 days.
Result:	Showed marked tumor growth inhibition with treatment/control (T/C) ratios of 51% and 19%, respectively.

IC 50

EGFR: 1.1-8.0 nM (IC₅₀)

References

[1] Hasako S, et al. TAS6417, A Novel EGFR Inhibitor Targeting Exon 20 Insertion Mutations. Mol Cancer Ther. 2018 Aug;17(8):1648-1658. DOI:10.1158/1535-7163.MCT-17-1206
[2] Hibiki Udagawa, et al. TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. Mol Cancer Res. 2019 Nov;17(11):2233-2243. DOI:10.1158/1541-7786.MCR-19-0419

TAS6417 Preparation Products And Raw materials

Raw materials

Preparation Products

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TAS6417 Suppliers

China 122 India 1 United States 2 Global 125

Suzhou Ryan Pharmaceutical Technology Co., Ltd.

Tel: 0512-68780025 18962125825
Email: sales@ryanchem.com
Country: China
ProdList: 169
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Jinan Chuanbei Biotechnology Co., Ltd

Tel: 18654547380; 15269175648
Fax: 0531-67802093
Email: qingyan7590@163.com
Country: China
ProdList: 17
Advantage: 58

Shanghai Hope Chem Co., Ltd.，

Tel: +21-18501659228 18501659228
Fax: sales@hope-chem.com
Email: info@hope-chem.com
Country: China
ProdList: 492
Advantage: 55

Chunchuang (Wuhan) Technology Co., Ltd

Tel: 15727060112
Email: yutianchun2007@126.com
Country: China
ProdList: 9856
Advantage: 58

Twochem Co.Ltd

Tel: 021-021-58111628 15800915896
Fax: QQ 3285589261
Email: sales@twochem.com
Country: China
ProdList: 304
Advantage: 55

Anqing Benro pharmachem Technology Co.,Ltd.

Tel: 05565209906 15391842992
Email: 794263564@qq.com
Country: China
ProdList: 126
Advantage: 58

Changzhou Borl Biotechnology Co.,LTD

Tel: 13606124132;13656121842
Email: luyan0021@163.com
Country: China
ProdList: 240
Advantage: 58

TargetMol Chemicals Inc.

Tel: 021-021-33632979 15002134094
Fax: 021-33632979
Email: marketing@targetmol.com
Country: China
ProdList: 8000
Advantage: 58

ShangHai Caerulum Pharma Discovery Co., Ltd.

Tel: 18149758185 18149758185
Email: sales-cpd@caerulumpharma.com
Country: China
ProdList: 3505
Advantage: 58

Bide Pharmatech Ltd.

Tel: 400-400-164-7117 18317119277
Fax: +86-21-61629029
Email: product02@bidepharm.com
Country: China
ProdList: 40000
Advantage: 60

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View Lastest Price from TAS6417 manufacturers

HangZhou RunYan Pharma Technology Co.,LTD.

Product: TAS6417;Zipalertinib;CLN-081 1661854-97-2
Price: US $0.00-0.00/g
Min. Order: 1g
Purity: 99% HPLC
Supply Ability: 10000
Release date: 2024-09-19

1661854-97-2, TAS6417Related Search:

Ziprasidone Hydrochloride Futibatinib GLPG-1690 TAS0728 TAS-102 TAS-301 TAS-116

TAS6417

TAS-6417;TAS 6417;TAS6417

(S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide

2-Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]-

CLN-081

TAS6417 TAS-6417

Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]- (ACI)

Zipalertinib (TAS-6417)

2-Propenamide, N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizi

TAS-6417,EGFR,ErbB-1,TAS6417,PC-9,lung,Inhibitor,Apoptosis,CLN081,BEAS-2B,CLN 081,cancer,BID007,CLN-081,inhibit,TAS 6417,NSCLC,H1975,Epidermal growth factor receptor,BID019,HER1,Akt

Zipalertinib

(S)-N-[4-Amino-6-methyl-5-(3-quinolyl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl]acrylamide

N-[(8S)-4-amino-8,9-dihydro-6-methyl-5-(3-quinolinyl)pyrimido[5,4-b]indolizin-8-yl]-2-propenamide

TAS6417, 10 mM in DMSO

TAS6417/Zipalertinib

1661854-97-2

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