BP-1-102

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种口服生物可利用的 STAT3 小分子抑制剂，Kd 为 504 nM。

An orally bioavailable, small-molecule inhibitor of STAT3 with Kd of 504 nM; blocks Stat3-pTyr peptide interactions and Stat3 activation at 4-6.8 uM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells; suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and KLF8, blocks Stat3-NF-κB cross-talk, and enhances E-cadherin expression; inhibits growth of human breast and lung tumor xenografts.

BP-1-102 binds Stat3 with an affinity KD of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8.

Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth.

BP-1-102 | BP1-102 | BP 1-102 | BP1102

JAK/STAT Signaling

STAT

STAT3

Cancer

——

1334493-07-0

626.5915

C29H27F5N2O6S

>98% (HPLC)

DMSO: ≥ 33 mg/mL

O=C(O)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1O

Benzoic acid, 4-[[(4-cyclohexylphenyl)methyl][2-[methyl[(2,3,4,5,6-pentafluorophenyl)sulfonyl]amino]acetyl]amino]-2-hydroxy-

(-20℃)

With Ice Pack

≥ 2 years