ibrutinib

Ibrutinib (PCI-32765) 是一种布鲁顿酪氨酸激酶 (BTK) 抑制剂 (IC50=0.5 nM)，具有不可逆性和选择性。Ibrutinib 可以阻断 BTK 抑制 B 细胞的增殖和存活，具有抗肿瘤活性，可以用于治疗慢性淋巴细胞白血病等。

Ibrutinib D5 is a deuterium-labeled Ibrutinib. Ibrutinib is an irreversible Btk inhibitor.

N-piperidine Ibrutinib hydrochloride 是一种强效的 BTK 抑制剂，是BTK 配体，抑制 WT BTK 和 C481S BTK ，可用于合成一系列 PROTAC 分子。N-piperidine Ibrutinib hydrochloride具有潜在的抗癌活性，可抑制癌细胞的生长和增殖。

Ibrutinib is a selective, irreversible Btk inhibitor (IC50: 0.5 nM). Ibrutinib Racemate is the racemate of Ibrutinib.

Ibrutinib Interm 0441 is a piperidine derivative with an amine protecting group and may be used in the preparation of biologically active compounds.

N-piperidine Ibrutinib 是一种有效的 BTK 抑制剂，对 WT BTK 和 C481S BTK 的 IC50 分别为 51.0 和 30.7 nM。它可作为BTK 配体用于一系列PROTAC 的合成，如SJF620。 SJF620 是一种有效的 PROTAC BTK 降解剂，DC50 为 7.9 nM。

Ibrutinib dimer is an impurity of Ibrutinib. IIbrutinib dimer is a Dimer of Ibrutinib. Ibrutinib is an irreversible Btk inhibitor (IC50: 0.5 nM).

Ibrutinib-MPEA is ibrutinib derivative. Ibrutinib is a covalent and irreversible BTK inhibitor that has been used to treat hematological malignancies.

Ibrutinib-biotin is a probe that consists of Ibrutinib linked to biotin via a long chain linker, has an IC50 of 0.755-1.02 nM for BTK.

PCI 45227 is an active metabolite of the Bruton's tyrosine kinase inhibitor ibrutinib .1PCI 45227 is formed from ibrutinib by the cytochrome P450 (CYP) isoform CYP3A. 1.Veeraraghavan, S., Viswanadha, S., Thappali, S., et al.Simultaneous quantification of lenalidomide, ibrutinib and its active metabolite PCI-45227 in rat plasma by LC-MS/MS: Application to a pharmacokinetic studyJ. Pharm. Biomed. Anal.107151-158(2015)

Remibrutinib 是有效的、口服具有活力的 bruton tyrosine kinase 抑制剂 (IC50:1 nM)，在血液中抑制 BTK 活性的 IC50的值为 0.23 μM。它具有研究慢性荨麻疹的潜力。

Ibrutinib deacryloylpiperidine (IBT4A) 是 Ibrutinib 的杂质之一。它是一种不可逆的、选择性的 Btk 抑制剂 (IC50:0.5 nM)。

IBT6A 是一种 Ibrutinib 的杂质。它可用于合成 IBT6A-Ibrutinib 二聚体和 IBT6A 加合物。Ibrutinib 是不可逆的选择性 Btk 抑制剂 (IC50:0.5 nM)。

(Rac)-IBT6A hydrochloride is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in the synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a Btk inhibitor (IC50: 0.5 nM).

IBT6A hydrochloride, an impurity of Ibrutinib, is relevant for synthesizing IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a Btk inhibitor (IC50: 0.5 nM).

(Rac)-IBT6A 是 IBT6A 的外消旋体。 IBT6A 是依鲁替尼的杂质，可用于 IBT6A 依鲁替尼二聚体和 IBT6A 加合物的合成。

Propargyl-PEG1-acid, a PEG-based PROTAC linker, enables the synthesis of BTK-CRBN PROTACs, specifically Ibrutinib-based PROTAC 4 and PROTAC 5. At a concentration of 10 μM, PROTAC 5 facilitates the degradation of BTK and induces the degradation of CSK, LYN, and LAT2[1].

Propargyl-PEG4-acid is a PEG-based PROTAC linker can be used in the synthesis of BTK-IAP PROTACs Ibrutinib -based PROTAC 2 and an analogue PROTAC 3. PROTAC 3 causes BTK degradation with a DC50 of 200 nM in THP-1 cells[1].

Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.

Abivertinib, also known as AC0010 and Avitinib, is a third-generation EGFR tyrosine kinase inhibitor and BTK Inhibitor that demonstrated clinical efficacy and manageable adverse events (AEs). Abivertinib inhibits cell proliferation, reduces colony-forming capacity, and induces apoptosis and cell cycle arrest in AML cells, especially those harboring FLT3-ITD mutations. Abivertinib was also found to be more sensitive than ibrutinib in treating AML. Abivertinib may be a promising novel agent for AML, with potential for combination treatment with HHT.

GNE-431 is a potent, selective and noncovalent Btk inhibitor with IC50 of 3.2 nM. GNE-431 showed excellent potency against the C481R, T474I, and T474M mutants. GNE-431 may provide a treatment option to patients, especially those who have acquired resistance to ibrutinib by mutation of Cys481 or Thr474.

BTK-IN-22 是一种BTK 抑制剂 (IC50: 12.8 nM)。BTK-IN-22 还抑制 BLX 和 BMX，IC50分别为 35.6 和 5.7 nM。与 Ibrutinib 相比，BTK-IN-22 显示出更高的激酶选择性。

BTK-IN-23 是一种BTK 抑制剂 (IC50: 12.8 nM)。BTK-IN-23 还抑制 BLX 和 BMX，IC50分别为 35.6 和 5.7 nM。与 Ibrutinib 相比，BTK-IN-23 显示出更高的激酶选择性。

(Rac)-IBT6A hydrochloride 是 IBT6A hydrochloride 的消旋体。IBT6A 是 Ibrutinib 的一种杂质。IBT6A 可用于合成 IBT6A-Ibrutinib 二聚体和 IBT6A 加合物。Ibrutinib 是一种不可逆的选择性 Btk 抑制剂，IC50为 0.5 nM。