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RO4929097 - ≥98%, high purity , Gamma-secretase inhibitor, CAS No.847925-91-1, Gamma-secretase inhibitor

Item Number
R127403
Grouped product items
SKUSizeAvailabilityPrice Qty
R127403-5mg
5mg
In stock
$107.90
R127403-10mg
10mg
In stock
$195.90
R127403-25mg
25mg
In stock
$441.90
R127403-50mg
50mg
In stock
$608.90
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View related series
presenilin 1 Inhibitor

Basic Description

SynonymsKK8645V7LE | RG-4733 | RO4929097 | 847925-91-1 | RO-4929097 | Ro 4929097 | (S)-2,2-dimethyl-N1-(6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl)-N3-(2,2,3,3,3-pentafluoropropyl)malonamide | N1-[(7S)-6,7-dihydro-6-oxo-5H-dibenz[b,d]azepin-7-yl]-2,2-dimethyl-N3-(2,2,3,3,3-p
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological Mechanisms

RO4929097 is an orally bioavailable, small-molecule gamma secretase (GS) inhibitor with an IC50 of 4 nM. It binds to GS and blocks activation of Notch receptors, which may inhibit tumor cell proliferation. RO4929097 inhibits Notch process

Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionGamma-secretase inhibitor

Product Properties

ALogP4.6

Associated Targets(Human)

PSEN1 Tchem Presenilin-1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
A549 (127892 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
APH1A Tbio Gamma-secretase (4915 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name 2,2-dimethyl-N-[(7S)-6-oxo-5,7-dihydrobenzo[d][1]benzazepin-7-yl]-N'-(2,2,3,3,3-pentafluoropropyl)propanediamide
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
InChi Key OJPLJFIFUQPSJR-INIZCTEOSA-N
Canonical SMILES CC(C)(C(=O)NCC(C(F)(F)F)(F)F)C(=O)NC1C2=CC=CC=C2C3=CC=CC=C3NC1=O
Isomeric 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
PubChem CID 49867930
Molecular Weight 469.4

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4 results found

Lot NumberCertificate TypeDateItem
I2224526Certificate of AnalysisJul 10, 2024 R127403
I2224527Certificate of AnalysisJul 10, 2024 R127403
I2224528Certificate of AnalysisJul 10, 2024 R127403
I2224529Certificate of AnalysisJul 10, 2024 R127403

Chemical and Physical Properties

SolubilityDMSO 94 mg/mL Water <1 mg/mL Ethanol 16 mg/mL

Related Documents

 SDS

 Specification Sheet

References

1. Huynh C, Poliseno L, Segura MF, Medicherla R, Haimovic A, Menendez S, Shang S, Pavlick A, Shao Y, Darvishian F et al..  (2011)  The novel gamma secretase inhibitor RO4929097 reduces the tumor initiating potential of melanoma..  PLoS ONE,  6  (9): (e25264).  [PMID:21980408]
2. Tolcher AW, Messersmith WA, Mikulski SM, Papadopoulos KP, Kwak EL, Gibbon DG, Patnaik A, Falchook GS, Dasari A, Shapiro GI et al..  (2012)  Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors..  J Clin Oncol,  30  (19): (2348-53).  [PMID:22529266]
3. Strosberg JR, Yeatman T, Weber J, Coppola D, Schell MJ, Han G, Almhanna K, Kim R, Valone T, Jump H et al..  (2012)  A phase II study of RO4929097 in metastatic colorectal cancer..  Eur J Cancer,  48  (7): (997-1003).  [PMID:22445247]

Solution Calculators

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