LY2801653
- Product Name
- 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
- Formula Weight
- 552.53
- MOL File
- 1206799-15-6.mol
LY2801653 Property
- Boiling point:
- 795.3±60.0 °C(Predicted)
- 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
- InChI
- InChI=1S/C30H22F2N6O3/c1-17-3-9-23(30(40)38(17)22-7-4-20(31)5-8-22)29(39)36-21-6-10-27(25(32)12-21)41-28-11-18-16-35-37(2)26(18)13-24(28)19-14-33-34-15-19/h3-16H,1-2H3,(H,33,34)(H,36,39)
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Danger
- Hazard statements
-
H302Harmful if swallowed
H351Suspected of causing cancer
H360May damage fertility or the unborn child
H372Causes damage to organs through prolonged or repeated exposure
- Precautionary statements
-
P201Obtain special instructions before use.
P202Do not handle until all safety precautions have been read and understood.
P260Do not breathe 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.
P281Use personal protective equipment as required.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P308+P313IF exposed or concerned: Get medical advice/attention.
P314Get medical advice/attention if you feel unwell.
P330Rinse mouth.
P405Store locked up.
P501Dispose of contents/container to..…
N-Bromosuccinimide Price
- Product number
- 25978
- Product name
- LY2801653
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $62
- Updated
- 2024/03/01
- Product number
- 25978
- Product name
- LY2801653
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $180
- Updated
- 2024/03/01
- Product number
- 25978
- Product name
- LY2801653
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $330
- Updated
- 2024/03/01
- Product number
- 25978
- Product name
- LY2801653
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $893
- Updated
- 2024/03/01
- Product number
- A3573
- Product name
- LY2801653
- Packaging
- 100mg
- Price
- $900
- Updated
- 2021/12/16
LY2801653 Chemical Properties,Usage,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
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View Lastest Price from LY2801653 manufacturers
- Product
- LY2801653 1206799-15-6
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 97%-99.9%
- Supply Ability
- 100kg
- Release date
- 2019-12-25