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ML 786 dihydrochloride

Catalog #: 5036
1 Citation Datasheet / COA / SDS

Discontinued Product

5036 has been discontinued.
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ML 786 dihydrochloride | CAS No. 1237536-18-3 | Raf Kinase Inhibitors
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Description: Potent Raf kinase inhibitor; orally bioavailable
Alternative Names: BGB659

Chemical Name: 3-(1-Amino-1-methylethyl)-N-[(2R)-1,2,3,4-tetrahydro-7-oxo-1,8-naphthryridin-4-yl)oxy]-2-naphthalenyl]-5-benzamide dihydrochloride

Purity: ≥98%

Product Details
Citations (1)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

Potent Raf kinase inhibitor (IC50 values are 2.1, 2.5 and 4.2 nM for B-RafV600E, C-Raf and wild-type B-Raf respectively). Also inhibits Abl-1, DDR2, EPHA2 and RET tyrosine kinase activity. Inhibits pERK formation and attenuates tumor growth in melanoma cell xenografts expressing the B-RafV600E mutation in vivo. Orally bioavailable.

Technical Data

M.Wt:
611.48
Formula:
C29H29F3N4O3.2HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
1237536-18-3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Alkaline Phosphatase Controls Lineage Switching of Mesenchymal Stem Cells by Regulating the LRP6/GSK3? Complex in Hypophosphatasia
    W Liu, L Zhang, K Xuan, C Hu, L Li, Y Zhang, F Jin, Y Jin
    Theranostics, 2018;8(20):5575-5592.
  2. Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors.
    Gould et al.
    J.Med.Chem., 2011;54:1836
  3. Acquired JHDM1D-BRAF fusion confers resistance to FGFR inhibition in FGFR2-amplified gastric cancer.
    Sase et al.
    Mol.Cancer Ther., 2018;17:2217
  4. Identification of a potent and selective covalent Pin1 inhibitor
    BJ Pinch, ZM Doctor, B Nabet, CM Browne, HS Seo, ML Mohardt, S Kozono, X Lian, TD Manz, Y Chun, S Kibe, D Zaidman, D Daitchman, ZC Yeoh, NE Vangos, EA Geffken, L Tan, SB Ficarro, N London, JA Marto, S Buratowski, S Dhe-Pagano, XZ Zhou, KP Lu, NS Gray
    Nat. Chem. Biol., 2020;0(0):.

Product Datasheets

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Citation for ML 786 dihydrochloride

The citations listed below are publications that use Tocris products. Selected citations for ML 786 dihydrochloride include:

1 Citation: Showing 1 - 1

  1. Acquired JHDM1D-BRAF fusion confers resistance to FGFR inhibition in FGFR2- amplified gastric cancer.
    Authors: Sase Et al.
    Mol.Cancer Ther.  2018;

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