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Bfl-1-IN-6 TFA salt form · salt · Parent Bfl-1-IN-6 TFA

Bfl-1-IN-6 TFA is a Covalent, Orally Bioavailable, and Selective BFL1 Inhibitor.

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

Research area Cancer
Purity >98% Stock Inquire

Bfl-1-IN-6 TFA structure

CAS No.: 3106364-91-1

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
10 mg USD 760.00 BP-02179A-10mg In stock Get quote
25 mg USD 1,520.00 BP-02179A-25mg In stock Get quote
50 mg USD 2,430.00 BP-02179A-50mg In stock Get quote
100 mg USD 3,800.00 BP-02179A-100mg In stock Get quote
250 mg USD 7,800.00 BP-02179A-250mg In stock Get quote

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Description

Bfl-1-IN-6 TFA is a Covalent, Orally Bioavailable, and Selective BFL1 Inhibitor.

Biological activity

In Vitro Bfl-1-IN-6 (Compound 20) TFA induces caspase activation in SUDHL1 cells treated with 0.5 μM AZD5991 (HY-101533) with an EC50 of 350 nM, thereby resulting in decreased cell viability. Bfl-1-IN-6 TFA combined with 0.5 μM AZD5991 reduces the viability of SUDHL1 cells, with an EC50 of 250 nM, and causes no significant off-target toxicity in BFL1-deficient Karpas-422 cells. Bfl-1-IN-6 (0.3-9 μM; 6 h) TFA induces dose-dependent BFL1 stabilization and activation of cleaved caspase-3 in OCILY10 cells, and exhibits targeted apoptotic activity after 6 hours of treatment. In Vivo Bfl-1-IN-6 (Compound 20) (100-300 mg/kg; p.o.; single dose) TFA causes dose-dependent stabilization of BFL1 and activation of cleaved caspase 3 in OCILY10 lymphoma tumor xenografts in mice.

Identifiers

SMILES
C(C(O)=O)(F)(F)F.N([C@@H](C)C1=CC=C(Cl)C=C1)(C(C=C)=O)C2=CC(F)=C(O[C@@H]3CC[C@@H](N)C3)C=C2
InChIKey
HJRLDGALXMTJAU-QULYPMOISA-N

Specifications

MW (average)
516.9130
Formula
C24H25ClF4N2O4
CAS No.
3106364-91-1
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℃, 3 years; In solvent -20℃ 1 month;

Solubility

soluble in DMSO

References

[1]. Palisse A, et al. Structure-Based Discovery of a Series of Covalent, Orally Bioavailable, and Selective BFL1 Inhibitors. Journal of medicinal chemistry. 2024 Dec 26;67(24):22055-22079.

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