Product Name :
CBP/p300-IN-5
Description:
P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.8 nM.
CAS:
1889284-33-6
Molecular Weight:
618.55
Formula:
C29H27F5N6O4
Chemical Name:
2-[(3’R,4S)-3′-fluoro-5′-1-[(methylcarbamoyl)methyl]-1H-pyrazol-4-yl-2,5-dioxo-2′,3′-dihydrospiro[imidazolidine-4,1′-inden]-1-yl]-N-[(4-fluorophenyl)methyl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]acetamide
Smiles :
C[C@H](N(CC1=CC=C(F)C=C1)C(=O)CN1C(=O)[C@@]2(C[C@@H](F)C3C=C(C=CC2=3)C2=CN(CC(=O)NC)N=C2)NC1=O)C(F)(F)F
InChiKey:
SWXCHCQCWFXILM-DAXQEMQKSA-N
InChi :
InChI=1S/C29H27F5N6O4/c1-16(29(32,33)34)39(12-17-3-6-20(30)7-4-17)25(42)15-40-26(43)28(37-27(40)44)10-23(31)21-9-18(5-8-22(21)28)19-11-36-38(13-19)14-24(41)35-2/h3-9,11,13,16,23H,10,12,14-15H2,1-2H3,(H,35,41)(H,37,44)/t16-,23+,28-/m0/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.Talazoparib Data Sheet
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.Macitentan In Vivo
Additional information:
P300/CBP-IN-5 is a potent p300/CBP histone acetyltransferase inhibitor extracted from patent WO2016044770A1, Example 715, has an IC50 of 18.PMID:31794287 8 nM.|Product information|CAS Number: 1889284-33-6|Molecular Weight: 618.55|Formula: C29H27F5N6O4|Chemical Name: 2-[(3’R,4S)-3′-fluoro-5′-1-[(methylcarbamoyl)methyl]-1H-pyrazol-4-yl-2,5-dioxo-2′,3′-dihydrospiro[imidazolidine-4,1′-inden]-1-yl]-N-[(4-fluorophenyl)methyl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]acetamide|Smiles: C[C@H](N(CC1=CC=C(F)C=C1)C(=O)CN1C(=O)[C@@]2(C[C@@H](F)C3C=C(C=CC2=3)C2=CN(CC(=O)NC)N=C2)NC1=O)C(F)(F)F|InChiKey: SWXCHCQCWFXILM-DAXQEMQKSA-N|InChi: InChI=1S/C29H27F5N6O4/c1-16(29(32,33)34)39(12-17-3-6-20(30)7-4-17)25(42)15-40-26(43)28(37-27(40)44)10-23(31)21-9-18(5-8-22(21)28)19-11-36-38(13-19)14-24(41)35-2/h3-9,11,13,16,23H,10,12,14-15H2,1-2H3,(H,35,41)(H,37,44)/t16-,23+,28-/m0/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|P300/CBP-IN-5 inhibits p300 LnCap-FGC cellls proliferation with an IC50 of 14.8 nM. P300/CBP-IN-5 inhibits H3K27Ac with an IC50 value of 4.6 nM in PC-3 cells.|In Vivo:|The effect of P300/CBP-IN-5 (Example 715) on tumor growth is evaluated in subcutaneous, SuDHL-8 (B-cell lymphoma) and 22RV1 (prostate) xenograft tumors implanted in SCID female mice. Human cancer cells are inoculated subcutaneously into the right hind flank of female SCID mice on study day 0. Administration of P300/CBP-IN-5 (7.5 mg/kg/day) is initiated at the time of size match. P300/CBP-IN-5 induces significant tumor growth inhibition in multiple xenograft tumor models (the tumor growth inhibition of 62% in SuDHL-8 xenograft tumor model; 48% in 22RV1 xenograft tumor model).|Products are for research use only. Not for human use.|
