brk

AZ7550 trimesylate salt (AZ7550 Mesylate) 是奥希替尼的活性代谢产物，AZ7550 trimesylate salt 抑制 IGF1R 活性，可用于研究非小细胞肺癌。

AZ7550 是 AZD9291 的活性代谢物，可抑制 IGF1R 活性，IC50为 1.6 μM。

XMU-MP-2 是一种有效和选择性的蛋白酶抑制剂，具有抗癌活性，在小鼠异种移植模型中 抑制致癌 BRK 驱动的肿瘤的生长。

Spebrutinib (LMK-435) 是一种共价的、高效的、选择性的、具有口服活性的Btk 抑制剂 (IC50:0.5 nM)。

SB-633825 can inhibit cancer cell growth and angiogenesis. SB-633825 is an effective and ATP-competitive inhibitor of TIE2, LOK, and BRK (IC50s: 3.5 nM, 66 nM, 150 nM, respectively).

Tilfrinib 是一种有效的选择性乳腺肿瘤激酶(Brk)抑制剂（IC50 = 3.15 nM），具有抗增殖和抗肿瘤活性。

BRK inhibitor P21d hydrochloride is a highly potent inhibitor of breast tumor kinase (BRK PTK6), displaying an IC50 of 30 nM. Additionally, it effectively suppresses p-SAM68 with an IC50 value of 52 nM. This compound, BRK inhibitor P21d hydrochloride, serves as a valuable tool for evaluating the efficacy of BRK inhibitors in xenograft breast tumor models, enabling the assessment of their in vivo activity.

AZ7550 hydrochloride (AZ7550 hydrochloride ) 是 AZD9291 的活性代谢物，可抑制 IGF1R 活性，IC50为 1.6 μM。

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。

PLX-4720 是一种有效且选择性的 B-Raf (V600E) 抑制剂，旨在阻断致癌B-Raf的ATP结合位点，IC50为 13 nM。

GSK2656157 是一种ATP 竞争性的PERK 选择性抑制剂，IC50值为 0.9 nM。

PF-6689840是一种有效的选择性II 型PTK6 Brk 抑制剂,在生化检测中IC50为54 nM；在过表达PTK6 WT 的工程化HET293T 细胞中抑制Y342处的PTK6磷酸化,IC50为0.25 uM；表现出优异的激酶选择性,与I 型抑制剂相比；抑制肿瘤细胞生长,这与细胞中PTK6的表达水平无关。

P21d hydrochloride is a potent and selective breast tumor Ki nase (Brk) inhibitor (IC50 = 30 nM). Exhibits >650-fold selectively for Brk over Aurora B Ki nase and Lck. Downregulates SNAIL protein, restores E-cadherin expression and suppresses migration in breast cancer cells. Also activein vivoand orally bioavailable.

EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases including BRK, FGFR1, c-Kit, and PDGFRb.