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1352608-82-2 (EW-7197)

1

Identification

EW-7197 EW-7197
Name EW-7197
Formula C22H18FN7
MW 399.42
CAS No. 1352608-82-2
EINECS
Smiles CC1=CC=CC(C2=C(C3=CN4C(C=C3)=NC=N4)NC(CNC5=CC=CC=C5F)=N2)=N1
Synonyms EW7197;EW 7197; N-((5-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-4-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline
InChI InChI=1S/C22H18FN7/c1-14-5-4-8-18(27-14)22-21(15-9-10-20-25-13-26-30(20)12-15)28-19(29-22)11-24-17-7-3-2-6-16(17)23/h2-10,12-13,24H,11H2,1H3,(H,28,29)
2

Introduction

Background Information

EW-7197 is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. target: ALK4/ALK5 IC 50: 13 nM for TGF-β receptor ALK4, 11 nM for TGF-β receptor ALK5. [1] In vitro: EW-7197 inhibits TGFβ-induced Smad2 or Smad3 phosphorylation and the epithelial-to-mesenchymal transition (EMT) in TGFβ-treated breast cancer cells. In addition, EW-7197 also abrogates TGFβ1-induced tumor cell migration and invasion in breast cells. EW-7197 inhibited Smad/TGFβ signaling, cell migration, invasion, and lung metastasis in mouse mammary tumor virus. [2] In vivo: EW-7197 inhibition downregulates Smad4 in melanoma-bearing mice. EW-7197 induces ubiquitin-mediated degradation of Smad4 in melanoma-bearing mice. In a mouse B16 melanoma model, EW-7197 (2.5 mg/kg daily p.o.) suppresses the progression of melanoma with enhanced cytotoxic T-lymphocyte (CTL) responses. EW-7197 dissolved in artificial gastric fluid formulation (vehicle; ddH2O 900 ml, conc. HCl 7 ml, NaCl 2.0 g, pepsin 3.2 g) was given orally by feeding needle to mice from 4 days after inoculation. [3] ......by MedChemexpress Co., Ltd.
3

Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:Light yellow to yellow Solid EBNumber:EB000067149

Storage condition

Store in a tightly closed container, in a cool and dry place. by MedChemexpress Co., Ltd.

Solubility

10 mM in DMSO by CHEMSCENE, LLC
DMSO: 79 mg/mL (197.78 mM); Ethanol, 43 mg/mL warming (107.65 mM) by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways TGF-beta/Smad
Target TGF-β Receptor
Research Area Cancer
Indications
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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
EW-7197 - Phase 1 Clinical
EW-7197 - Phase 1
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Safety Data of EW-7197

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 2mg/USD90(In stock);5mg/USD130(In stock);10mg/USD220(In stock);25mg/USD440(In stock);50mg/USD680(In stock);100mg/USD950(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. China
10

Related Products

Other Forms of 1352608-82-2

Name CAS No Formula MW

Recommended Compounds in TGF-β Receptor

Name CAS No Formula MW
K 02288 1431985-92-0 C20H20N2O4 352.38
ML347 1062368-49-3 C22H16N4O 352.39
DMH-1 1206711-16-1 C24H20N4O 380.44
LDN-212854 1432597-26-6 C25H22N6 406.48
SB-505124 (hydrochloride) 356559-13-2 C20H22ClN3O2 371.86
A 77-01 607737-87-1 C18H14N4 286.33
SB-505124 694433-59-5 C20H21N3O2 335.4
LY-364947 396129-53-6 C17H12N4 272.3
LDN193189 (Hydrochloride) 1062368-62-0 C25H26Cl4N6 552.33
SD-208 627536-09-8 C17H10ClFN6 352.75
RepSox 446859-33-2 C17H13N5 287.32
LDN193189 1062368-24-4 C25H22N6 406.48
A 83-01 909910-43-6 C25H19N5S 421.52
LY2109761 700874-71-1 C26H27N5O2 441.52
LY2157299 700874-72-2 C22H19N5O 369.42
GW788388 452342-67-5 C25H23N5O2 425.48
SB 525334 356559-20-1 C21H21N5 343.42
SB-431542 301836-41-9 C22H16N4O3 384.39
R-268712 879487-87-3 C20H18FN5O 363.39
ITD-1 1099644-42-4 C27H29NO3 415.52

Recommended Compounds in Same Indication

Name CAS No Formula MW
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Route of Synthesis

12

References

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More Information

EW-7197

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