A TNIK inhibitor
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NCB-0846

Item No. 33268

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cis-4-[[2-(1H-benzimidazol-6-ylamino)-8-quinazolinyl]oxy]-cyclohexanol
CAS Number
1792999-26-8
Molecular Formula
C21H21N5O2
Formula Weight
375.4
Purity
≥90%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 1 mg/mlDMSO: 5 mg/ml
λmax
222, 246, 293, 311 nm
SMILES
O[C@@H](CC1)CC[C@@H]1OC2=CC=CC3=C2N=C(NC4=CC=C(N=CN5)C5=C4)N=C3
InChi Code
InChI=1S/C21H21N5O2/c27-15-5-7-16(8-6-15)28-19-3-1-2-13-11-22-21(26-20(13)19)25-14-4-9-17-18(10-14)24-12-23-17/h1-4,9-12,15-16,27H,5-8H2,(H,23,24)(H,22,25,26)/t15-,16+
InChi Key
FYWRWBSYRGSWIQ-IYBDPMFKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $41

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    5 mg

    $178

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    25 mg

    $631

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    50 mg

    $970

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    Product Description

    NPC-0846 is an inhibitor of TRAF2- and NCK-interacting kinase (TNIK; IC50 = 21 nM).1 It is selective for TNIK over a panel of 46 kinases but does inhibit FLT3, JAK3, PDGFRα, TrkA, Cdk2/CycA2, and HGK by greater than 80% at 100 nM. NPC-0845 (3 µM) inhibits phosphorylation of transcription factor 4 (TCF4) and autophosphorylation of TNIK in cell-based assays. It inhibits the growth and colony formation of HCT116 colon cancer cells in two-dimensional growth and soft-agar assays, respectively, as well as reduces tumor growth in an HCT116 mouse xenograft model. NPC-0846 (50 and 100 mg/kg) also reduces tumor growth in patient-derived xenograft (PDX) mouse models of colon cancer.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Masuda, M., Uno, Y., Ohbayashi, N., et al. TNIK inhibition abrogates colorectal cancer stemness. Nat. Commun. 7, 12586 (2016).