96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode

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Product Description

Description & Advantages

    • A unique collection of 137 tyrosine kinase inhibitors for high throughput screening (HTS) and high content screening (HCS)
    • Bioactivity and safety confirmed by preclinical research and clinical trials
    • Some tyrosine kinase inhibitors have been approved by FDA
    • Targets tyrosine kinases such as EGFR, VEGFR, SRC, c-Met and JAK
    • Structurally diverse, medicinally active and cell permeable
    • Rich documentation with structure, IC50 and customer reviews
    • NMR and HPLC to ensure the high purity

Product Details

Formulation: A collection of 137 inhibitors supplied as pre-dissolved DMSO solutions
Container: 96 Well Format Sample Storage Tube With Screw Cap and Optional 2D Barcode
Stability:
3 months -20°C in DMSO
6 months -80°C in DMSO
Shipping: Blue ice
Packaging: Inert gas

Tyrosine Kinase Inhibitor Library Contents

Download the Tyrosine Kinase Inhibitor Library - XLSX Download the Tyrosine Kinase Inhibitor Library - SDF

Contents are for reference only and are subject to change without notice.

Tyrosine Kinase Inhibitor Library Composition

Kinase Inhibitor Library Composition

Customer Reviews (10)

AS-605240 Review
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Source Nature,2011, 478(7369):349-55. Sunitinib Malate purchased from Selleck
Method Western immunoblots
Cell Lines Mouse pancreatic stem cells
Concentrations 12 uM
Incubation Time 2 days
Results Increased Ezh2 expression and β-cell BrdU incorporation were eliminated by simultaneous treatment with the receptor tyrosine kinase inhibitors Sunitinib.

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Source Nature, 2011, 478(7369):349-55. Sunitinib Malate purchased from Selleck
Method Immunofluorescent staining
Cell Lines Mouse pancreatic stem cells
Concentrations 12 uM
Incubation Time 2 days
Results Compared to vehicle-exposed controls, juvenile islets exposed to PDGF-AA had a sixfold increase of β-cell BrdU incorporation, an effect eliminated by simultaneous exposure to Sunitinib or U0126.

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Source Science, 2011, 331(6019), 912-6. PD173074 purchased from Selleck
Method Immunohistochemistry
Cell Lines uterine horn
Concentrations
Incubation Time
Results The epithelia of vehicle-treated horn showed prominent expression of p-FRS2 and p-ERK1/2 (Fig. A, a and c). However, the levels of both p-FRS2 and p-ERK1/2 were reduced in the epithelia of PD173074-treated horn on day 4 of pregnancy (Fig. A, b and d). We also observed a marked decline in the proliferative activity of Hand2-null uterine epithelia, as indicated by decreased Ki-67 staining (Fig. A, e and f). Administration of either PD173074 (Fig. C, a to d) or PD184352 (Fig. C, e to h) to Hand2-null uterine horns blocked the phosphorylation of epithelial ER a at Ser118 and the expression of Muc-1.

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Source Nat Genet, 2012, 44(8):852-60. Erlotinib HCl (OSI-744) purchased from Selleck
Method Western blot
Cell Lines HHCC827 ER1 and ER2 cells
Concentrations 0.1 uM
Incubation Time 48 h
Results It sought to validate genetic findings using pharmacologic inhibitors of AXL. As expected, erlotinib decreased pEGFR, pERK, pAKT, pRelA and increased the levels of cleaved Parp in parental HCC827 cells irrespective of concurrent treatment with MP-470. In contrast, these effects of erlotinib treatment were observed only upon concurrent treatment with MP-470 in the HCC827 ER1 and ER2 cells.

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Source Nat Med , 2011, 17, 1116-1120. Crizotinib (PF-02341066) purchased from Selleck
Method Western blot
Cell Lines RCT-E565 transplanted tumors
Concentrations 25 mg/kg/d, 50 mg/kg/d
Incubation Time 0-21 d
Results We then treated mice bearing RCT-E565 tumor transplants with PF02341066, a c-Met inhibitor currently in clinical development. PF02341066 abrogated both p-Akt and p-S6RP signals as well as tumor growth.

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Source Cancer Cell, 2012, 22(5), 656-667 . Ponatinib (AP24534) purchased from Selleck
Method Western blot
Cell Lines RCH-ACV cells
Concentrations 50 nM
Incubation Time 1-24 h
Results Treatment of these cells with a CSK inhibitor (BMS-599626) or a BTK inhibitor (PCI-32765) did not recapitulate the dasatinib/ponatinib phenotype.

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Source Cancer Cell , 2011, 19, 679–690. Crizotinib (PF-02341066) purchased from Selleck
Method Cell Growth Inhibition Assay
Cell Lines Ba/F3 cells
Concentrations
Incubation Time 48 h
Results The sensitivities of L1196M-driven Ba/F3 cell clones to PF-02341066 were lower, closely resembling that of the Ba/F3 parental cells. The therapeutic indexes of CH5424802 and PF-02341066, the IC50 ratio of EML4-ALK L1196M-driven cell clones to the parental cells, were 7- to 12-fold and 1- to 2-fold.

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Source Cancer Discov, 2014, 4(7), 816-27. Cabozantinib (XL184, BMS-907351) purchased from Selleck
Method Western blot
Cell Lines A-375 melanoma cells
Concentrations 3 uM
Incubation Time
Results XL184 combined with PLX4720, compared to PLX 4720 alone, abrogated AXL-mediated induction of AKT phosphorylation and rescue of ERK phosphorylation but had no effect on AKT or ERK levels in A-375 cell lines.

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Source Cancer Discov, 2013, 3(6), 636-47. PD173074 purchased from Selleck
Method Western blot
Cell Lines SW780 cells
Concentrations 10, 40 mg/kg
Incubation Time
Results Similar results for FGFR fusion-positive lines were obtained in vivo. SW780 xenografts exhibited decreased tumor growth with increasing doses of PD173074.

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Source Cancer Discov, 2013, 3, 224-37. Neratinib (HKI-272) purchased from Selleck
Method Colony assays
Cell Lines MCF10A cells
Concentrations 0.5 μmol/L
Incubation Time a week
Results Treatment with lapatinib and neratinib inhibited the growth of these invasive colonies.

Product Citations (21)

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Tags: phosphatase inhibitor library