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RO4929097

CAT: 0013-GTR19161465-03Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19161465-03Size:5 mg
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Description
RO4929097 (RG 4733) is a potent, selective, orally active γ-secretase inhibitor with IC50 of 4 nM, inhibits Notch processing in the Notch cell-based reporter assay with IC50 of 5 nM; displays >100-fold selectivity against a panel of 75 other proteins of various types including receptors, ion channels and enzymes; inhibits Notch processing in human tumor-derived cells, inhibits the production of ICN, reducing the expression of the downstream Notch target Hes1 in A549 cells; demonstrates in vivo efficacy in A549 xenograft model.Lung Cancer Phase 2 Discontinued (In Vitro) :RO4929097 inhibits the production of ICN reducing the expression of the downstream Notch target, Hes1, producing a less transformed morphology in A549 cells. RO4929097 inhibits Notch processing in human tumor-derived cells. RO4929097 (1 μM) inhibits the growth of breast cancer cells, and the inhibition is 20% for SUM149 and 10% for SUM190 cells. RO4929097 does not have a marked effect in invasiveness of SUM149 cells. RO4929097 significantly reduces colony formation by both cell lines with the effect being more notable in SUM149 than by SUM190 cells. RO4929097 inhibits proliferation, anchorage independent growth, and sphere formation of primary melanoma cells in vitro. (In Vivo) :RO4929097 (3-60 mg/kg, p.o.) results in significant tumor growth inhibition in nude mice bearing A549 NSCLC xenografts, compared with vehicle-treated animals. When mice are treated with 60 mg/kg RO4929097 twice daily with the 7+/14- schedule, treatment initially causes regression of established A549 tumors. RO4929097 impairs the growth of primary melanoma cells in vivo. The percentage of secondary tumors formed by RO4929097-treated cells is lower; the secondary tumors formed by RO4929097-treated cells are smaller; a significant delay in tumor formation by the RO4929097-treated cells compared to the vehicle-treated ones is observed in mice injected with 104 cells in vivo.
CAS Number
847925-91-1
Product Name Alternative
RG 4733 | RO 4929097
Purity
>98% (HPLC)
Solubility
DMSO: ≥ 49 mg/mL
Smiles
O=C (N[C@H]1C2=CC=CC=C2C3=CC=CC=C3NC1=O) C (C) (C) C (NCC (F) (F) C (F) (F) F) =O
Molecular Formula
C22H20F5N3O3
Molecular Weight
469.4045
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Propanediamide, N1-[ (7S) -6,7-dihydro-6-oxo-5H-dibenz[b, d]azepin-7-yl]-2,2-dimethyl-N3- (2,2,3,3,3-pentafluoropropyl) -

Chemical Information

Ro 4929097

RO4929097 is a member of the class of dibenzoazepines that is the amide formed from formal condensation of the carboxy group of 2,2-dimethyl-3-oxo-3-[(2,2,3,3,3-pentafluoropropyl)amino]propanoic acid with the amino group of (7S)-7-amino-5,7-dihydrodibenzo[b,d]azepin-6-one. It has a role as an EC 3.4.23.46 (memapsin 2) inhibitor. It is a lactam, a dicarboxylic acid diamide, an organofluorine compound and a dibenzoazepine.

CAS Number847925-91-1
PubChem CID49867930
IUPAC Name2,2-dimethyl-N-[(7S)-6-oxo-5,7-dihydrobenzo[d][1]benzazepin-7-yl]-N'-(2,2,3,3,3-pentafluoropropyl)propanediamide
Molecular FormulaC22H20F5N3O3
Molecular Weight469.4
XLogP4.6
Topological Polar Surface Area87.3
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count8
Rotatable Bond Count5
Heavy Atom Count33
Formal Charge0
Complexity771
SMILES
CC(C)(C(=O)NCC(C(F)(F)F)(F)F)C(=O)N[C@H]1C2=CC=CC=C2C3=CC=CC=C3NC1=O
InChI
InChI=1S/C22H20F5N3O3/c1-20(2,18(32)28-11-21(23,24)22(25,26)27)19(33)30-16-14-9-4-3-7-12(14)13-8-5-6-10-15(13)29-17(16)31/h3-10,16H,11H2,1-2H3,(H,28,32)(H,29,31)(H,30,33)/t16-/m0/s1
InChIKey
OJPLJFIFUQPSJR-INIZCTEOSA-N
Chemical Structure
2D Structure
2D structure of Ro 4929097
CAS: 847925-91-1
CID: 49867930
Formula: C22H20F5N3O3
MW: 469.4
Interactive 3D Structure
Loading 3D structure...
View on PubChemRaw 3D data
Computed Properties
PropertyValue
Molecular Weight469.4
XLogP34.6
Hydrogen Bond Donor Count3
Hydrogen Bond Acceptor Count8
Rotatable Bond Count5
Exact Mass469.14248232
Monoisotopic Mass469.14248232
Topological Polar Surface Area87.3 Ų
Heavy Atom Count33
Formal Charge0
Complexity771
Isotope Atom Count0
Defined Atom Stereocenter Count1
Undefined Atom Stereocenter Count0
Defined Bond Stereocenter Count0
Undefined Bond Stereocenter Count0
Covalently-Bonded Unit Count1
Compound Is CanonicalizedYes

Alternative Products

CatalogName
A4005-SRO4929097

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