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Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

ACK1

ACK1 (Activated Cdc42-associated Kinase 1), also known as TNK2, is a non-receptor tyrosine kinase activated by Cdc42, involved in regulating cell migration, proliferation, and survival. It influences signaling pathways like RAS and NF-kB, and plays a key role in cytoskeletal remodeling and cell adhesion. Overexpression of ACK1 is linked to cancer metastasis, making it a potential therapeutic target for cancer treatment.

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Vemurafenib

T2382918504-65-1

Vemurafenib (RG7204) is a B-RAF inhibitor that inhibits RAFV600E and c-RAF-1 (IC50=31 48 nM) selectively and potently. Vemurafenib exhibits antitumor activity and is used for the treatment of BRAF V600E mutation-positive melanoma.

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Cited

GNF-7

T3196839706-07-9

GNF-7 is Bcr-Abl WT and Bcr-Abl T315I inhibitor with IC50 of 133 nM and 61 nM, respectively.

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AIM-100

T5092873305-35-2

AIM-100 is a Ack1 inhibitor (IC50: 24 nM).

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AZ7550

T135641421373-99-0

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

$133

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KRCA-0008

T26411472795-20-2

KRCA-0008 is an effective and specific ALK Ack1 inhibitor (IC50: 12 4 nM); displays drug-like properties without hERG liability.

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(R)-9b

T2017761655527-68-6

(R)-9b is an effective inhibitor of the ACK1 tyrosine kinase (IC50=56 nM) and exhibits anticancer activity. It selectively targets ACK1 but also inhibits kinases in the JAK family, specifically JAK2 and Tyk2. (R)-9b is used in research related to hormone-regulated cancers, such as prostate cancer and breast cancer.

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10-14 weeks

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