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Chemical Structure| 1446144-04-2 Chemical Structure| 1446144-04-2

Structure of CPI-203
CAS No.: 1446144-04-2

Chemical Structure| 1446144-04-2

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CPI 203 is a potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).

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Product Details of CPI-203

CAS No. :1446144-04-2
Formula : C19H18ClN5OS
M.W : 399.90
SMILES Code : O=C(N)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
MDL No. :MFCD27997886
InChI Key :QECMENZMDBOLDR-AWEZNQCLSA-N
Pubchem ID :71291068

Safety of CPI-203

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

Related Pathways of CPI-203

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD4, IC50:37 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
HepG2.2.15 5 μM 24-48 h CPI-203 significantly inhibited IFN-γ-induced PD-L1 expression Cancer Sci. 2022 Jan;113(1):28-40
HepG2.2.15 5 μM 48 h CPI-203 significantly inhibited IFN-γ-induced PD-L1 expression Cancer Sci. 2022 Jan;113(1):28-40
c-Kit+ cells 0.5 μM 24 h To test the expression changes of MYC target genes, a subset of MYC target genes was down-regulated Genes Dev. 2015 Sep 15;29(18):1915-29
LSK CD150+CD48− HSCs 0.5 μM 24 h To validate the activity of CPI-203 in HSCs, Myc mRNA expression was reduced by 2-3 fold Genes Dev. 2015 Sep 15;29(18):1915-29
MDA-MB-231 1, 2, 5 μM 48 h CPI-203 could inhibit PD-L1 expression in the absence of IFN-γ stimulation Cancer Sci. 2022 Jan;113(1):28-40
MDA-MB-231 1, 2, 5 μM 48 h CPI-203 could inhibit PD-L1 expression in the absence of IFN-γ stimulation Cancer Sci. 2022 Jan;113(1):28-40
DT-28 50 μM 72 h Vitamin C pretreatment reduced the EC50 of CPI-203, enhancing its efficacy against TNBC cells. EBioMedicine. 2019 May;43:201-210
HCC1937 50 μM 72 h Vitamin C pretreatment reduced the EC50 of CPI-203, enhancing its efficacy against TNBC cells. EBioMedicine. 2019 May;43:201-210
BT-549 50 μM 72 h Vitamin C pretreatment reduced the EC50 of CPI-203, enhancing its efficacy against TNBC cells. EBioMedicine. 2019 May;43:201-210
MDA-MB-231 50 μM 72 h Vitamin C pretreatment reduced the EC50 of CPI-203, enhancing its efficacy against TNBC cells. EBioMedicine. 2019 May;43:201-210
SK-MEL-2 1 μM 72 h To evaluate the inhibitory effect of CPI-203 on melanoma cell proliferation. Results showed that CPI-203 significantly enhanced the inhibition of SK-MEL-2 melanoma cell proliferation after ascorbate pretreatment. Cancer Res. 2018 Jan 15;78(2):572-583.
SK-MEL-28 1 μM 72 h To evaluate the inhibitory effect of CPI-203 on melanoma cell proliferation. Results showed that CPI-203 significantly enhanced the inhibition of SK-MEL-28 melanoma cell proliferation after ascorbate pretreatment. Cancer Res. 2018 Jan 15;78(2):572-583.
C8161 1 μM 72 h To evaluate the inhibitory effect of CPI-203 on melanoma cell proliferation. Results showed that CPI-203 significantly enhanced the inhibition of C8161 melanoma cell proliferation after ascorbate pretreatment. Cancer Res. 2018 Jan 15;78(2):572-583.
1205Lu 1 μM 72 h To evaluate the inhibitory effect of CPI-203 on melanoma cell proliferation. Results showed that CPI-203 significantly enhanced the inhibition of 1205Lu melanoma cell proliferation after ascorbate pretreatment. Cancer Res. 2018 Jan 15;78(2):572-583.
A2058 1 μM 72 h To evaluate the inhibitory effect of CPI-203 on melanoma cell proliferation. Results showed that CPI-203 significantly enhanced the inhibition of A2058 melanoma cell proliferation after ascorbate pretreatment. Cancer Res. 2018 Jan 15;78(2):572-583.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Ergfl/fl and Ergfl/fl; Mx1Cre mice Intraperitoneal injection 5 mg/kg Twice daily for 1 week CPI-203 partially rescued the HSC defect caused by Erg deletion, restoring HSC numbers Genes Dev. 2015 Sep 15;29(18):1915-29

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.50mL

0.50mL

0.25mL

12.50mL

2.50mL

1.25mL

25.01mL

5.00mL

2.50mL

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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