PFI-1
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MedKoo CAT#: 406261

CAS#: 1403764-72-6

Description: PFI-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs with acetylated histone tails. Co-crystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts.


Price and Availability

Size
Price

10mg
USD 150
100mg
USD 650
1g
USD 2750
Size
Price

25mg
USD 250
200mg
USD 950
2g
USD 3950
Size
Price

50mg
USD 450
500mg
USD 1850
5g
Ask price

PFI-1, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide). Shipping fee: from $30.00 (USA); from $45.00 (Canada); from $70.00 (international).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 406261
Name: PFI-1
CAS#: 1403764-72-6
Chemical Formula: C16H17N3O4S
Exact Mass: 347.09398
Molecular Weight: 347.39
Elemental Analysis: C, 55.32; H, 4.93; N, 12.10; O, 18.42; S, 9.23


Synonym: PFI1; PFI 1; PFI-1

IUPAC/Chemical Name: 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide

InChi Key: TXZPMHLMPKIUGK-UHFFFAOYSA-N

InChi Code: InChI=1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20)

SMILES Code: O=S(C1=CC=CC=C1OC)(NC2=CC3=C(NC(N(C)C3)=O)C=C2)=O


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Picaud S, Da Costa D, Thanasopoulou A, Filippakopoulos P, Fish PV, Philpott M, Fedorov O, Brennan P, Bunnage ME, Owen DR, Bradner JE, Taniere P, O'Sullivan B, Muller S, Schwaller J, Stankovic T, Knapp S. PFI-1 - A highly Selective Protein Interaction Inhibitor Targeting BET bromodomains. Cancer Res. 2013 Apr 10. [Epub ahead of print] PubMed PMID: 23576556.

2: Fish PV, Filippakopoulos P, Bish G, Brennan PE, Bunnage ME, Cook AS, Federov O, Gerstenberger BS, Jones H, Knapp S, Marsden B, Nocka K, Owen DR, Philpott M, Picaud S, Primiano MJ, Ralph MJ, Sciammetta N, Trzupek JD. Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit. J Med Chem. 2012 Nov 26;55(22):9831-7. doi: 10.1021/jm3010515. Epub 2012 Nov 8. PubMed PMID: 23095041; PubMed Central PMCID: PMC3506127.

3: Moore KN, Tian C, McMeekin DS, Thigpen JT, Randall ME, Gallion HH. Does the progression-free interval after primary chemotherapy predict survival after salvage chemotherapy in advanced and recurrent endometrial cancer?: a Gynecologic Oncology Group ancillary data analysis. Cancer. 2010 Dec 1;116(23):5407-14. doi: 10.1002/cncr.25480. Epub 2010 Aug 24. PubMed PMID: 20737572.