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Cat. No.: HY-122703

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BETi-211

BETi-211 is an orally active, selective BET inhibitor with a K_i < 1 nM. BETi-211 inhibits BET function as epigenetic readers by binding to BET proteins (BRD2, BRD3, and BRD4). BETi-211 suppresses the growth of various triple-negative breast cancer (TNBC) cell lines, with an IC₅₀ < 1 μM. BETi-211 can be utilized to synthesize PROTAC molecules designed to degrade BET proteins. BETi-211 is applicable for research into TNBC.

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

CAS No.: 1995867-02-1
Formula: C₂₆H₂₉N₇O₃
Molecular Weight:487.55

Storage:

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

Data Sheet (293 KB)

BETi-211 Chemical Structure

CAS No.: 1995867-02-1

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

BET

< 1 nM (Ki)

BRD2

BRD4

BRD3

All Epigenetic Reader Domain Isoforms :

In Vitro

Anti-cancerCell Cycle RegulationApoptosisOthers

Anti-cancer

BETi-211 (4 days) inhibits the growth of TNBC cell lines, with an IC₅₀ <1 µM in 9 out of 13 cell lines^[1].
BETi-211 (1 µM; 3-8 h) upregulates the mRNA and protein expression of BRD2 and MCL1 in TNBC cell lines (MDA-MB-231, MDA-MB-468).^[1].

Anti-cancer

Cell Cycle Regulation

Apoptosis

BETi-211 (1 µM; 24-48 h) induces cell cycle arrest (with a reduction in S-phase cells) and moderate apoptosis in TNBC cell lines (such as MDA-MB-468)^[1].

Others

In biochemical assays, BETi-211 binds to BET proteins with a K_i <1 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-468 and TNBC cell lines
Concentration:

1 µM
Incubation Time:

1 h, 3 h, 8 h
Result:

Did not degrade BET proteins but upregulated BRD2 and MCL1.

Real Time qPCR^[1]

Cell Line:

MDA-MB-157, MDA-MB-231, MDA-MB-468 cells
Concentration:

1 µM
Incubation Time:

3, 8 h
Result:

Caused mixed up- and down-regulation of genes.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-468 cells
Concentration:

1 µM
Incubation Time:

48 h
Result:

Elicited only modest apoptosis induction.

In Vivo

Anti-cancer

BETi-211 (50 mg/kg; p.o.; once daily, 5 days per week; 2-3 weeks) inhibits tumor growth in SCID mouse models bearing human triple-negative breast cancer (TNBC) xenografts (WHIM24 PDX, MDA-MB-453, MDA-MB-231, and MDA-MB-468)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SCID mice were injected subcutaneously with WHIM24 PDX, MDA-MB-453, MDA-MB-231, and MDA-MB-468 cells^[1]
Dosage:

50 mg/kg
Administration:

p.o.; once daily, 5 days per week; 2, 3 weeks
Result:

Effectively suppressed breast tumor growth at well-tolerated dosing schedules.
Did not cause significant weight loss or apparent toxicity in the mice.

Related Protocols :

Breast Cancer Modeling

Chemical Information

CAS No. 1995867-02-1
Molecular Weight 487.55
Formula C₂₆H₂₉N₇O₃
SMILES

COCC1=NC(NC2=CC(C3CC3)=NN2CC)=C4C(NC5=C4C=C(OC)C(C6=C(C)ON=C6C)=C5)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (293 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Bai L, et al. Targeted degradation of BET proteins in triple-negative breast cancer. Cancer research. 2017 May 1;77(9):2476-87.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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BETi-211

All Epigenetic Reader Domain Isoforms

Biological Activity

Description

IC50 & Target

In Vitro

In Vivo

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

BETi-211 Related Classifications

HY-122703 Related Classifications

Bioz

Keywords

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