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  3. CZL-077

CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research.

For research use only. We do not sell to patients.

CZL-077

CZL-077 Chemical Structure

CAS No. : 3032444-06-4

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Description

CZL-077 is a potent, selective, and orally active p300/CBP bromodomain (BRD) inhibitor (p300 IC50 = 0.034 μM, CBP IC50 = 0.052 μM) exhibiting high selectivity over the BRDs of BET proteins (BRD2/3/4). CZL-077 inhibits cell growth with IC50 values of 0.024 μM and 5.6 μM in OPM-2 and 22RV1 cells, respectively. CZL-077 shows antitumor efficacy in OPM-2 and 22RV1 xenograft mouse models. CZL-077 can be used for multiple myeloma and prostate cancer research[1].

IC50 & Target[1]

BRD2 (BD1)

3.81 μM (IC50)

BRD2 (BD2)

>10 μM (IC50)

BRD3 (BD1)

5.54 μM (IC50)

BRD3 (BD2)

>10 μM (IC50)

BRD4 BD1

6.45 μM (IC50)

BRD4 BD2

>10 μM (IC50)

p300

0.034 μM (IC50)

CBP

0.052 μM (IC50)

Molecular Weight

577.62

Formula

C30H26F3N5O2S

CAS No.
SMILES

CC1=NC(CC2)=C(S1)C[C@@H]2N3C([C@H]4N(C5=CC=C(F)C(F)=C5)C([C@@H](F)C4)=O)=NC6=CC(C7=C(C)ON=C7C)=CC=C63

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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CZL-077
Cat. No.:
HY-180804
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