ARV-771

SKU: orb1301792

Description

ARV-771 is a potent PROTAC-based degrader of BET proteins, exhibiting high affinity for BRD2, BRD3, and BRD4 bromodomains with Kd values in the single-digit nanomolar range. This compound is a valuable chemical probe for investigating BET protein function in cancer research, demonstrating efficacy in both cellular assays and in vivo tumor models.

Research Area

Epigenetics & Chromatin, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	1949837-12-0
MW	986.64
Purity	99.69% (May vary between batches)
Formula	C₄₉H₆₀ClN₉O₇S₂
SMILES	CC=1C2=C(N3C([C@H](CC(NCCOCCCOCC(N[C@H](C(=O)N4[C@H](C(N[C@@H](C)C5=CC=C(C=C5)C=6SC=NC6C)=O)C[C@@H](O)C4)C(C)(C)C)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C
Target	Epigenetic Reader Domain,PROTACs
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.03 mM);DMSO:10 mM

Bioactivity

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Target IC50	BRD2(1):34 nM (Kd)\|BRD3(1):8.3 nM (Kd)\|BRD4(1):9.6 nM (Kd)\|BRD4(2):7.6 nM (Kd)\|BRD3(2):7.6 nM (Kd)\|BRD2(2):4.7 nM (Kd)
In Vivo	METHODS: Nude mice successfully bearing transplanted HepG2 cell tumors were randomly divided into two groups and treated with ARV-771 (20 mg/kg/day, subcutaneous injection) every other day for 25 days. Tumor volume and body weight of mice were measured every 5 days. Immediately after extraction of xenografts from mice, tumor weight was measured by an electronic balance. RESULTS After ARV-771 treatment, tumor volume and tumor weight were significantly reduced. Immunochemical detection results showed that ARV-771 reduced the expression of Ki67 and increased the expression of cleaved Caspase 3 in xenograft tissues. Read more...
In Vitro	METHODS: ARV-771 (0.01/0.025/0.05/0.1/0.25/0.5/1/2μM) was used to culture Hep3B, HepG and HCCLM3 cells to observe whether ARV-771 inhibits the growth of these cancer cells. RESULTS ARV-771 had a dose-dependent inhibition on cancer cell viability when the concentration reached 0.25 μM in Hep3B and HepG2 cells and 0.5 μM in HCCLM3 cells. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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inhibit, EpigeneticReaderDomain, Epigenetic Reader Domain, Inhibitor, ARV 771, ARV771, ARV-771, BET, PROTACs

Quality Guarantee

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Compound Identifiers

PubChem CID

126619980 ↗

Key Properties

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No computed properties available.

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ARV-771 (orb1301792)

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Purity:	99.18% (May vary between batches)
CAS Number:	1948273-03-7
MW:	481.05
Formula:	C₂₃H₃₃ClN₄O₃S

Purity:	99.86% (May vary between batches)
CAS Number:	1948273-02-6
MW:	444.59
Formula:	C₂₃H₃₂N₄O₃S

MW:	517.51
Formula:	C₂₃H₃₄Cl₂N₄O₃S

Purity:	>98%
CAS Number:	1948273-03-7
MW:	413.4
Formula:	C₂₁H₁₈F₃N₅O

ARV-771

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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ARV-771 (orb1301792)

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