CPI-0610 free base · Synonyms: Pelabresib

CPI-0610 is a potent, selective, and cell-active BET inhibitor.

For research use only. Not for human or veterinary use.

Target Epigenetic Reader Domain

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

CPI-0610 structure

CAS No.: 1380087-89-7

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 450.00	BP-01878-100mg	In stock	Get quote
250 mg	USD 750.00	BP-01878-250mg	In stock	Get quote
500 mg	USD 1,150.00	BP-01878-500mg	In stock	Get quote
1 g	USD 1,750.00	BP-01878-1g	In stock	Get quote
5 g	Inquire	BP-01878-5g	Inquire	Inquire

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Description

CPI-0610 is a potent, selective, and cell-active BET inhibitor. CPI-0610 inhibits BRD4-BD1 with an IC50 of 39 nM, and with an EC50 value of 0.18 μM for MYC.

Biological activity

In Vitro Pelabresib (0-1500 nM; 72 hours; Multiple myeloma cell lines and primary MM cells) treatment reduces the viability of MM cells in a dose-dependent manner. Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment leads to G1 cell cycle arrest. Pelabresib (800 nM; 72 hours; INA6 and MM.1S cells) treatment significantly increases apoptosis in MM cells after 72 hours. In Vivo Pelabresib (30-60 mg/kg; oral administration; for 28 days; MV-4-11 mouse xenograft model) treatment results in substantial suppression of tumor growth over the time period examined (41%, 80%, and 74% tumor growth inhibition, respectively), without any significant body weight loss in the animals.

Identifiers

SMILES: CC1=NOC2=C1C1=CC=CC=C1C(=N[C@H]2CC(N)=O)C1=CC=C(Cl)C=C1
InChIKey: GCWIQUVXWZWCLE-INIZCTEOSA-N

Specifications

MW (average): 365.8130
Formula: C₂₀H₁₆ClN₃O₂
CAS No.: 1380087-89-7
Physical state: Solid
Color: White to off-white
Shipping: 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: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Albrecht BK, et al. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J Med Chem. 2016 Feb 25;59(4):1330-9.

[2]. Siu KT, et al. Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma. Leukemia. 2017 Aug;31(8):1760-1769.

Same target

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Same research area

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