BET-IN-12

Cat. No.: HY-150516S: FAQs
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BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4[1].

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

BET-IN-12 Chemical Structure

CAS No. : 1800343-11-6

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Description

BET-IN-12 is an orally avtive inhibitor of bromodomain and extra-terminal (BET) with an IC50 of 0.9 nM for BRD4[1].

IC₅₀ & Target

0.9 nM (BRD4)^[1]

In Vitro

BET-IN-12 (compound 15) (24 hours) displays BRD4 and c-Myc inhibition, MM proliferation with IC₅₀s values of 0.9 nM, 2.0 nM, and 6.0 nM, respectively^[1].
BET-IN-12 (compound 15) (24 hours) has high oxidative stability across species and low glucuronidation across species, so that translate into low orally administered minimum efficacious doses (MEDs) ^[1].

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

In Vivo

BET-IN-12 (compound 15) is 100% oral bioavailability in mouse^[1].
BET-IN-12 (compound 15) impairs the growth of established PDX tumors (TGI = 88%) at MED = 2 mg/kg (AUC = 4800 nM•h)^[1].
pharmacokinetic (PK) profile^[1]

	dose (iv/po, mg/kg)	CL_p ((mL/min)/kg)	V_d (L/kg)	half-life (ie, h)	F (%)	AUC (po, nM^.h)
mouse	1.0/3.0	4.2	1.4	3.4	100	25000
rat	1.0/5.0	18	2.9	4.1	74	6600
dog	0.1/0.3	13	5.8	7.6	73	550
monkey	0.1/0.3	4.3	1.3	4.0	85	1900

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

Molecular Weight

516.62

Formula

C₃₀H₂₉D₃FN₅O₂

CAS No.

1800343-11-6

SMILES

CC(C)(O)C(C(F)=C1)=CC(N2[C@@H](C3CCOCC3)C4=CC=CC=C4)=C1C(N=C5)=C2C=C5C(N(N=N6)C)=C6C([2H])([2H])[2H]

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

Handling Instructions (2659 KB)

References

[1]. Hill, Matthew D., et al. Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties. ACS Med Chem Lett. 2022.

BET-IN-12 Related Classifications

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This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.

Keywords:

BET-IN-121800343-11-6Epigenetic Reader DomainbromodomainBET inhibitorgene transcriptioncancercarbolineInhibitorinhibitorinhibit

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