LY2801653
- CAS No.
- 1206799-15-6
- Chemical Name:
- LY2801653
- Synonyms
- CS-685;NSC32624;LY2801653;NSC 32624;NSC-32624;Merestinib;MET inhibitor;LY2801653(Merestinib);Merestinib(LY 2801653);MET INHIBITOR; LY2801653; LY-2801653; LY 2801653; MERESTINIB
- CBNumber:
- CB92650875
- Molecular Formula:
- C30H22F2N6O3
- Molecular Weight:
- 552.53
- MDL Number:
- MFCD23160048
- MOL File:
- 1206799-15-6.mol
Boiling point | 795.3±60.0 °C(Predicted) |
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Density | 1.42±0.1 g/cm3(Predicted) |
storage temp. | Store at -20°C |
solubility | ≥27.65 mg/mL in DMSO; insoluble in H2O; ≥5.02 mg/mL in EtOH with gentle warming and ultrasonic |
form | solid |
pka | 10.83±0.70(Predicted) |
color | White to yellow |
InChIKey | QHADVLVFMKEIIP-UHFFFAOYSA-N |
SMILES | C1(=O)N(C2=CC=C(F)C=C2)C(C)=CC=C1C(NC1=CC=C(OC2C(C3=CNN=C3)=CC3=C(C=2)C=NN3C)C(F)=C1)=O |
FDA UNII | 5OGS5K699E |
NCI Drug Dictionary | merestinib |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() ![]() GHS07,GHS08 |
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Signal word | Danger | |||||||||
Hazard statements | H360-H302-H351-H372 | |||||||||
Precautionary statements | P260-P264-P270-P314-P501-P264-P270-P301+P312-P330-P501-P201-P202-P281-P308+P313-P405-P501 | |||||||||
NFPA 704 |
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LY2801653 price More Price(22)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Cayman Chemical | 25978 | LY2801653 ≥98% | 1206799-15-6 | 1mg | $62 | 2024-03-01 | Buy |
Cayman Chemical | 25978 | LY2801653 ≥98% | 1206799-15-6 | 5mg | $180 | 2024-03-01 | Buy |
Cayman Chemical | 25978 | LY2801653 ≥98% | 1206799-15-6 | 10mg | $330 | 2024-03-01 | Buy |
Cayman Chemical | 25978 | LY2801653 ≥98% | 1206799-15-6 | 50mg | $893 | 2024-03-01 | Buy |
ApexBio Technology | A3573 | LY2801653 | 1206799-15-6 | 100mg | $900 | 2021-12-16 | Buy |
LY2801653 Chemical Properties,Uses,Production
Description
LY2801653 is an orally bioavailable MET kinase inhibitor (Ki = 2 nM). It also inhibits MST1R, Axl, MNK1/2, FLT3, DDR1, and DDR2 (IC50s = 11, 2, 7, 7, 0.1, and 7 nM, respectively, in a cell-based assay). It inhibits MET autophosphorylation stimulated by hepatocyte growth factor (HGF) in H460 and S114 cells (IC50s = 35.2 and 59.2 nM, respectively) and inhibits growth of Ba/F3 cells transfected with MET-activating mutations (IC50s = 12-248 nM). LY2801653 (0.01-10 μM) completely blocks cell scattering induced by HGF in DU145 cells. It reduces tumor growth in MET autocrine (U-87MG) and MET over-expression (H441) mouse xenograft models when administered at doses of 4 and 12 mg/kg.
Description
MET is a tyrosine kinase that leads to downstream activation of several pathways including RAS and MAPK.?As a result, it is quite possible that MET inhibition can be active in RAS mutant tumors and maybe associated with EGFR resistance in NSCLC.?Two MET inhibitors, tivantinib and onartuzumab, have been examined in KRAS mutant NSCLC with others in clinical trials at this time.
Clinical Use
Preclinical testing also has shown merestinib to inhibit several other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, and NTRK1/2/3.
target
c-MET
References
[1] yan s b et al. , ly2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against met, mst1r, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. invest new drugs. 2012, 31: 833-844.
LY2801653 Preparation Products And Raw materials
Raw materials
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 60 |
Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29825 | 58 |
Shaanxi Dideu Medichem Co. Ltd | 18192627656 | 1012@dideu.com | China | 2999 | 58 |
HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10522 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 | support@targetmol.com | United States | 19973 | 58 |
View Lastest Price from LY2801653 manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2022-04-29 | Merestinib
1206799-15-6
|
US $1.00-100.00 / g | 1g | 99.8%min | 25Kg | Shaanxi Dideu Medichem Co. Ltd | |
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2019-12-26 | LY2801653
1206799-15-6
|
US $1.00 / KG | 1KG | 97%-99.9% | 100kg | Career Henan Chemical Co |
-
- Merestinib
1206799-15-6
- US $1.00-100.00 / g
- 99.8%min
- Shaanxi Dideu Medichem Co. Ltd
-
- LY2801653
1206799-15-6
- US $1.00 / KG
- 97%-99.9%
- Career Henan Chemical Co