1. Stem Cell/Wnt
    MAPK/ERK Pathway
  2. Wnt
    MAP4K

NCB-0846 

Cat. No.: HY-100830 Purity: 98.27%
Handling Instructions

NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.

For research use only. We do not sell to patients.

NCB-0846 Chemical Structure

NCB-0846 Chemical Structure

CAS No. : 1792999-26-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 132 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 234 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 474 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 816 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg USD 1440 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

NCB-0846 is an orally available TNIK inhibitor with an IC50 of 21 nM.

IC50 & Target[1]

Wnt

 

TNIK

21 nM (IC50)

In Vitro

NCB-0846 has anti-Wnt activity. NCB-0846 binds to TNIK in an inactive conformation, and this binding mode seems to be essential for Wnt inhibition. NCB-0846 shows inhibitory activity against TNIK with an IC50 of 21 nM. NCB-0846 also inhibits FLT3, JAK3, PDGFRα, TRKA, CDK2/CycA2, and HGK. NCB-0846 induces faster migration of TCF4 phosphorylated by TNIK within a concentration range of 0.1-0.3 μM and completely inhibits the phosphorylation of TCF4 at a concentration of 3 μM. NCB-0846 inhibits HCT116 cell growth and shows much higher (-20-fold) inhibitory activity against colony formation by the same cells in soft agar[1].

In Vivo

NCB-0846 suppresses the growth of tumors established by inoculating HCT116 cells into immunodeficient mice. The expression of Wnt-target genes (AXIN2, MYC and CCND1) in xenografts is reduced following the administration of NCB-0846. NCB-0846 induces an increase in the sub-G1 cell population. Cleavage of poly (ADP-ribose) polymerase 1 indicates the induction of apoptosis[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.6637 mL 13.3184 mL 26.6368 mL
5 mM 0.5327 mL 2.6637 mL 5.3274 mL
10 mM 0.2664 mL 1.3318 mL 2.6637 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

Mice: NCB-0846 is suspended in DMSO/polyethylene glycol#400/30% 2-hydroxypropyl-β-cyclodextrin solution (10:45:45v/v). Five million HCT116 cells suspended in medium containing 25% Matrigel are inoculated into the subcutaneous tissues of 9-week-old female BALB/c nude mice. Mice are randomized according to tumour volume (9 mice per group). NCB-0846 was administered daily by oral gavage at 0 (vehicle alone), 40 or 80 mg/kg (body weight) BID (bis in die) for 14 days[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

375.42

Formula

C₂₁H₂₁N₅O₂

CAS No.

1792999-26-8

SMILES

O[[email protected]@H](CC1)CC[[email protected]@H]1OC2=CC=CC(C=N3)=C2N=C3NC4=CC=C(N=CN5)C5=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 30 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
NCB-0846
Cat. No.:
HY-100830
Quantity: