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A-485

CAT: 0013-GTR19217377-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19217377-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
A potent, selective and, cell and in vivo active p300/CBP catalytic inhibitor with IC50 of 9.8/2.6 nM; displays selectivity for p300/CBP over other HATs and histone methyltransferases in cells; dose-dependently decreases H3K27Ac in prostate adenocarcinoma PC-3 cells with EC50 of 73 nM; selectively inhibits proliferation in lineage-specific tumour types; inhibits the AR transcriptional program in both androgen-sensitive and castration-resistant prostate cancer and inhibits tumour growth in a castration-resistant xenograft model. (In Vitro) :A three-hour treatment of prostate adenocarcinoma PC-3 cells with A-485 results in a dose-dependent decrease in H3K27Ac, with a half maximal effective concentration (EC50) of 73 nM. Treatment with A-485 does not alter p300 or CBP protein levels.The broadest sensitivity is observed in haematological tumours, where A-485 exhibits potent activity in most multiple myeloma cell lines, and in a subset of acute myeloid leukaemia lines and non-Hodgkin’s lymphoma lines. A-485 induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines. (In Vivo) :After tumours are established in SCID male mice, twice daily intraperitoneal injections of A-485 induce 54% tumour growth inhibition after 21 days of dosing (P<0.005 as compare to vehicle control) . In addition, in tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels of MYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo. However, at 16 hours post-dosing on the seventh day, A-485 drug levels in the plasma and tumour are decreased as compare to 3 hours. A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen.
CAS Number
1889279-16-6
Product Name Alternative
A485 | A 485
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O=C (N1CC (N ([C@H] (C (F) (F) F) C) CC2=CC=C (F) C=C2) =O) [C@@]3 (OC1=O) CCC4=CC (NC (NC) =O) =CC=C43
Molecular Formula
C25H24F4N4O5
Molecular Weight
536.484
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
N- (4-fluorobenzyl) -2- ((R) -5- (3-methylureido) -2',4'-dioxo-2,3-dihydrospiro[indene-1,5'-oxazolidin]-3'-yl) -N- ((S) -1,1,1-trifluoropropan-2-yl) acetamide

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