Successful, we will reply to you quickly.

OK

Please select the quantity.

OK

Your message is being sent, please wait.

Close

test

Close

Send mail failed, please send again!

Close

Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Motesanib

HY-10228

(AMG 706; AMG-706)

Motesanib

Motesanib Chemical Structure

Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret.

Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO $55 In-stock
10 mg $50 In-stock
50 mg $160 In-stock
100 mg $280 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €54 In-stock
10 mg €49 In-stock
50 mg €157 In-stock
100 mg €274 In-stock
200 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Bulk Inquiry

Inquiry Information
Product name: Motesanib
Cat. No.: HY-10228

Motesanib Data Sheet

  • View current batch:

    Purity: 99.93%

  • Network Version

    DataSheet

    Pdf Version Network Version

    MSDS

    Pdf Version

    COA

    Pdf Version

    NMR

    Pdf Version

    LCMS

Customer View

Related Compound Libraries

Biological Activity of Motesanib

Motesanib (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret.
IC50 value:  2 nM/3 nM/6 nM/8 nM(VEGFR1/2/3/c-Kit) [1]
Target: pan-VEGFR; Kit
in vitro: Motesanib Diphosphate has broad activity against the human VEGFR family, and displays >1000 selectivity against EGFR, Src, and p38 kinase. Motesanib Diphosphate significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10 nM, while displaying little effect at bFGF-induced proliferation with an IC50 of >3,000 nM. Motesanib Diphosphate also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50 of 207 nM and 37 nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells [1]. Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib Diphosphate treatment significantly sensitizes the cells to fractionated radiation [2].
in vivo: Administration of Motesanib Diphosphate at 100 mg/kg significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib Diphosphate twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1 mg/kg and 4.9 mg/kg, respectively. Motesanib Diphosphate induces a dose-dependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells [1]. Administration of Motesanib Diphosphate in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma (HNSCC) xenograft models [2]. Motesanib Diphosphate treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen [3].

Protocol (Extracted from published papers and Only for reference)

More

Chemical Information

M.Wt 373.45 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C22H23N5O
CAS No 453562-69-1
Solvent & Solubility

10 mM in DMSO

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.6777 mL 13.3887 mL 26.7773 mL
5 mM 0.5355 mL 2.6777 mL 5.3555 mL
10 mM 0.2678 mL 1.3389 mL 2.6777 mL

Clinical Information of Motesanib

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Motesanib Amgen Inc Metastatic non small cell lung cancer 31-JUL-07 28-FEB-13 Phase 3 29-MAR-13
Amgen Inc Metastatic ovary cancer 31-JUL-07 31-DEC-13 Phase 2 12-NOV-13
Amgen Inc Solid tumor 31-DEC-05 31-JUL-12 Phase 2 12-OCT-12
Amgen Inc Fallopian tube cancer 31-JUL-07 31-DEC-13 Phase 2 12-NOV-13
Amgen Inc Peritoneal tumor 31-JUL-07 31-DEC-13 Phase 2 12-NOV-13
Amgen Inc Non-small-cell lung cancer 31-JUL-07 31-AUG-11 Phase 2 16-AUG-12

References on Motesanib

Other Forms

Inhibitor Kit

Related c-Kit , VEGFR Products

  • 2,4-Pyrimidinediamine with linker

    2,4-Pyrimidinediamine with linker is a patent compound in WO2013055780A1, Page 71; multikinase inhibitor and has a -NH2 terminal linker for further synthesis.

  • Altiratinib

    Altiratinib(DCC-2701) is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with a HGF antagonist in vitro.

  • Amuvatinib

    Amuvatinib (MP-470) is a potent and multi-targeted inhibitor of c-Kit, PDGFR(alpha) and Flt3 with IC50 of 10 nM, 40 nM and 81 nM, respectively.

  • Apatinib

    Apatinib(YN-968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM.

  • Axitinib

    Axitinib(AG013736) blocked phosphorylation of VEGFR-2 and VEGFR-3 with average IC50s of 0.2 and 0.1 to 0.3 nM.

  • AZD2932

    AZD2932 is a new series of quinazoline ether inhibitor which potently inhibits VEGFR-2 and PDGFR with IC50s of 4 nM/8 nM/ 7 nM for PDGFR(beta)/VEGFR-2/Flt-3.

  • BMS-690514

    BMS-690514 is a potent and selective inhibitor of epidermal growth factor receptor (EGFR), HER2, and HER4, as well as the VEGF receptor kinases.

  • BMS-794833

    BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7/15 nM; also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378.

  • c-Met inhibitor 2

    c-Met inhibitor 2 is a potent compound that has activity against cancers dependent upon Met activation and also has activity against cancers as a VEGFR inhibitor.

  • DCC-2618

    DCC-2618 is a small molecule inhibitor of c-Kit and PDGFR with IC50s of 6 nM/30 nM/13 nM for c-Kit/PDGFR(alpha)/PDGFR(beta) respectively.

MORE