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Chemical Structure| 1403764-72-6 Chemical Structure| 1403764-72-6
Chemical Structure| 1403764-72-6

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CAS No.: 1403764-72-6

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PFI-1 is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.

Synonyms: PF-06405761; PF-6405761

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Product Details of PFI-1

CAS No. :1403764-72-6
Formula : C16H17N3O4S
M.W : 347.39
SMILES Code : O=S(C1=CC=CC=C1OC)(NC2=CC3=C(NC(N(C)C3)=O)C=C2)=O
Synonyms :
PF-06405761; PF-6405761
MDL No. :MFCD22580416
InChI Key :TXZPMHLMPKIUGK-UHFFFAOYSA-N
Pubchem ID :71271629

Safety of PFI-1

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of PFI-1

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD4, IC50:0.22 μM

    BRD2, IC50:98 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
A10.6 cells 5 μM 72 h PFI-1 robustly increased GFP expression, indicating its ability to reactivate latent HIV-1 PMC5709369
MCF7 cells 500 μM 2 days PFI-1 inhibits BRD4 binding to super-enhancers, reducing CD47 expression PMC5382276
K-562 >20 μM PFI-1 showed weak antiproliferative effects on K-562 cells with a GI50 >20 μM PMC3673830
KASUMI-1 0.8 ± 1 μM PFI-1 showed antiproliferative effects on KASUMI-1 cells with a GI50 of 0.8 ± 1 μM PMC3673830
THP-1 4 ± 2 μM PFI-1 showed antiproliferative effects on THP-1 cells with a GI50 of 4 ± 2 μM PMC3673830
MV4;11 1.5 ± 1 μM PFI-1 showed antiproliferative effects on MV4;11 cells with a GI50 of 1.5 ± 1 μM PMC3673830
A549 cells 5 μM 48 h Combination of PFI-1 with SAHA in A549 cells reduced the expression of NRP2 and ZEB1. PMC5549304
H358 cells 5 μM 48 h PFI-1 treatment in H358 cells decreased PD-L1 and SEMA3C expression. When combined with TGF-β1, PFI-1 significantly reduced the expression of NRP2, PD-L1, SEMA3C, vimentin, and ZEB1. PMC5549304
PC9 2 μM 48 h PFI-1 restored CBX5 expression and resensitized EGFRi-resistant LUAD cells to EGFRi/BETi combination therapy. PMC9942844
HCC827 2 μM 48 h PFI-1 restored CBX5 expression and resensitized EGFRi-resistant LUAD cells to EGFRi/BETi combination therapy. PMC9942844
TZMbl cells 5 μM 48 h PFI-1 significantly increased luciferase expression, indicating its ability to activate HIV-1 LTR PMC5709369
Jurkat C11 cells 5 μM 72 h PFI-1 robustly increased GFP expression, indicating its ability to reactivate latent HIV-1 PMC5709369
Candida albicans 0.3-410μM To evaluate the inhibitory effect of PFI-1 on CaBdf1 BDs, the results showed that PFI-1 had poor inhibitory effect on CaBdf1 BDs, with IC50 values ranging from 0.3-410μM. PMC5454392
C9BAC primary cortical neurons 5 μM 24 h PFI-1 treatment significantly increased the expression of V1-V3 transcripts of the human mutant C9ORF72 gene in C9BAC primary cortical neurons, reduced poly(GP)-DPR inclusions, but enhanced intranuclear RNA foci. PMC7962347
SH-SY5Y LE90 cells 5 μM 24 h PFI-1 significantly enhanced luciferase reporter activity in SH-SY5Y LE90 cells, indicating its ability to increase C9ORF72 gene expression. PMC7962347

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice B-ALL xenograft model Intraperitoneal injection 50 mg/kg Four times per week for 3 weeks PFI-1 could not reach the effective dose in vivo, so (+)-JQ1 was used instead, which significantly reduced the expression of Aurora B and c-Myc PMC3673830
Mice Human EGFR-mutant LUAD xenograft model Oral 2.5 mg/kg 3 times per week until the end of the experiment Combination treatment with PFI-1 and EGFRi significantly inhibited the growth of EGFRi-resistant LUAD tumors. PMC9942844
Mice Breast cancer model Intraperitoneal injection 20 mg/kg Three times per week for two weeks To evaluate the anti-tumour effect of PFI-1 in breast cancer, results showed that PFI-1 had no significant anti-tumour effect PMC8647932

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.88mL

0.58mL

0.29mL

14.39mL

2.88mL

1.44mL

28.79mL

5.76mL

2.88mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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