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Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

ROS Kinase

Proto-oncogene tyrosine-protein kinase ROS is an enzyme that in humans is encoded by the ROS1 gene. ROS Kinase is highly expressed in a variety of tumor cell lines, belongs to the sevenless subfamily of tyrosine kinase insulin receptor genes. The protein encoded by this gene is a type I integral membrane protein with tyrosine kinase activity. The protein may function as a growth or differentiation factor receptor.

Filter HomeSignaling PathwaysTyrosine Kinase/AdaptorsROS Kinase

Lorlatinib

T30611454846-35-5

Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.

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Entrectinib

T36781108743-60-7

Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1 3 5 12 7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity.

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Zidesamtinib

T729532739829-00-4

Zidesamtinib (NVL-520) is an orally active, selective, potent, and blood-brain-barrier-crossing inhibitor of ROS1 fusion and resistance mutations, inhibits ROS1 and ROS1 G2032R, and can be used in the study of non-small-cell lung cancer and solid tumors.

$163

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Merestinib

T34551206799-15-6

Merestinib (LY2801653) is an orally available, small molecule inhibitor of the proto-oncogene c-Met (Ki: 2 nM) with potential antineoplastic activity. Merestinib electively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing the constitutively activated c-Met protein.

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Crizotinib

T1661877399-52-5

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.

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Crizotinib hydrochloride

T83991415560-69-8

Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met, with IC50 values of 20 nM and 8 nM, respectively.

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Repotrectinib

T40711802220-02-5

Repotrectinib (TPX-0005) is a potent ALK ROS1 TRK inhibitor, with IC50 values of 1.01 nM for WT ALK, 5.3 nM for SRC, 1.08 nM for ALK L1196M, and 1.26 nM for ALK G1202R.

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Taletrectinib

T223181505515-69-4

Taletrectinib (AB-106) is a new-generation selective inhibitor of ROS1 NTRK including ROS1,NTRK1,NTRK2 and NTRK3 with IC50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM, respectively.

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Salvigenin

TMS174319103-54-9

Salvigenin is a potent hMAO-A inhibitor, has neuroprotective, antitumor and immunomodulatory effects.

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Iruplinalkib

T640281854943-32-0

Iruplinalkib (WX-0593) is an orally active, selective and potent ALK and ROS1 tyrosine kinase inhibitor with anticancer activity for use in the study of non-small cell lung cancer.

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Uniconazole

T2148283657-22-1

Uniconazole is a plant growth regulator that inhibit cytochrome P450 707As (Ki=68 nM). CYP707As is a major ABA catabolic enzyme that catabolize Abscisic acid, accordingly suppress gibberellin and sterol biosynthesis.

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F-1

T112542244775-31-1

F-1 is IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways.

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ROS-generating agent 1

T777622369030-41-9

Ros-generating agent 1 has anticancer activity and generates ROS by covalently modifying Sec-498 residues of TrxR. ROS-generating agent 1 reduces intracellular TrxR protein levels and promotes ROs-dependent apoptosis and ferroptosis in NCI-H460 cells.

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Taletrectinib free base

T389951505514-27-1

Taletrectinib free base (AB-106 free base) is a novel potent, selective and orally active ROS1 NTRK inhibitor.Taletrectinib free base has potent inhibitory effects on recombinant ROS1, NTRK1, NTRK2, and NTRK3, with IC50s of 0.207, 0.622, 2.28 and 0.98 nM, respectively, Taletrectinib free base also inhibited ROS1 G2032R and other Crizotinib-resistant ROS1 mutations.

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ROS kinases-IN-1

T60220370096-57-4

ROS kinases-IN-1 is a ROS tyrosine kinase inhibitor with IC50 value of 1.22 μM. ROS kinases-IN-1 shows anti-tumor activity.

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ROS kinases-IN-2

T74671687576-28-9

ROS kinases-IN-2, with an inhibition rate of 21.53% at 10 μM, is a potent ROS kinase inhibitor with potential anticancer activity and applications in studying abnormal cell growth.

$156

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PRDX1-IN-1

T78785

PRDX1-IN-1 is a selective and potent PRDX1 inhibitor with potential anti-inflammatory and anticancer activity for the study of breast and esophageal cancer.

$599

7-10 days

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APG-2449

T793632196186-84-0

APG-2449, an orally active inhibitor of ALK, ROS1, and FAK, demonstrates antitumor efficacy in mouse models of non-small cell lung cancer (NSCLC) [1].

$1,520

8-10 weeks

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Methyl 12-methyltridecanoate

T791595129-58-8

Methyl 12-methyltridecanoate ((R)-betaxolol hydrochloride), a biosurfactant derived from Brevibacterium casei LS14, enhances the biocompatibility of functionalized silver nanoparticles in vivo [1].

35 days

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Anti-inflammatory agent 64

T83048

Anti-inflammatory agent 64 (compound 4b) demonstrates antioxidant and anti-inflammatory properties, effectively inhibiting IL-6 and TNF-α secretion and reducing paw edema [1] in both in vitro and in vivo studies.

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ROS1-IN-2

T899122120337-16-6

ROS1-IN-2 (Compound 3), a ROS1 inhibitor, is utilized in cancer research.

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10-14 weeks

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HS-291

T82171

HS-291, a HtpG inhibitor targeting Borrelia burgdorferi (Bb), comprises BX-2819 (high affinity for Bb HtpG), a PEG linker, and Verteporfin (a photoactive toxin). Upon light activation, HS-291 generates reactive oxygen species that oxidize HtpG and selectively inactivate nearby proteins, leading to the rapid and irreversible inactivation of Bb [1].

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