2. Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR JAK/STAT Signaling Apoptosis
  3. FLT3 ERK Akt STAT Apoptosis
  4. UNC1666

UNC1666 is an ATP-competitive dual-target Mer/Flt3 tyrosine kinase inhibitor with IC50 values of 0.55 nM and 0.69 nM, and Ki values of 0.16 nM and 0.67 nM, respectively. UNC1666 reduces the phosphorylation levels of Mer and Flt3, suppresses downstream pro-survival signaling pathways (Erk1/2, Akt and Stat), induces cell apoptosis, and decreases colony formation of acute myeloid leukemia cells. UNC1666 is applicable to research related to acute myeloid leukemia.

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

UNC1666

UNC1666 Chemical Structure

CAS No. : 1429882-12-1

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

UNC1666 Related Antibodies

Top Publications Citing Use of Products

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

View All Akt Isoform Specific Products:

View All Isoforms
Akt Akt1 Akt2 Akt3

View All STAT Isoform Specific Products:

View All Isoforms
STAT3 STAT5 STAT6 STAT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

UNC1666 is an ATP-competitive dual-target Mer/Flt3 tyrosine kinase inhibitor with IC50 values of 0.55 nM and 0.69 nM, and Ki values of 0.16 nM and 0.67 nM, respectively. UNC1666 reduces the phosphorylation levels of Mer and Flt3, suppresses downstream pro-survival signaling pathways (Erk1/2, Akt and Stat), induces cell apoptosis, and decreases colony formation of acute myeloid leukemia cells. UNC1666 is applicable to research related to acute myeloid leukemia[1][2].

In Vitro

UNC1666 (Analogue 2) exhibits subnanomolar to low nanomolar in vitro inhibitory activity against Mer, Flt3, Axl (29 nM) and Tyro3 (37 nM) kinases, with the most potent activity against Flt3 (0.69 nM) and Mer (0.93 nM)[1].
UNC1666 (10-300 nM) inhibits Mer phosphorylation in Kasumi-1 AML cells in a concentration-dependent manner, and potently suppresses Flt3 phosphorylation in MV4;11 Flt3-ITD AML cells[2].
UNC1666 (50-300 nM) dose-dependently inhibits the downstream pro-survival signaling pathways (Erk1/2, Akt, and Stat) in Mer-positive Kasumi-1 cells and Flt3-ITD MV4;11 AML cells following 2 h of treatment, with stronger activity observed in Flt3-ITD cells[2].
UNC1666 (10-300 nM; 72 h) induces apoptosis in Mer-positive and Flt3-ITD AML cell lines in a dose-dependent manner after 72 hours of treatment[2].
UNC1666 (50-300 nM; 72 h) inhibits the long-term rebound growth of Kasumi-1 and MV4;11 acute myeloid leukemia (AML) cells even after the completion of treatment[2].
UNC1666 (10-300 nM; 72 h) significantly reduces the colony-forming ability of Mer-positive and Flt3-ITD AML cell lines cultured in soft agar[2].
UNC1666 (50-300 nM; 2 h) dose-dependently inhibits the phosphorylation of Mer and Flt3 in primary AML blasts co-expressing Mer and Flt3ITD, suppresses downstream pro-survival signaling pathways (Erk1/2, Akt, Stat5) in the cells, induces cellular apoptosis, and reduces colony-forming ability[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

UNC1666 Related Antibodies

Apoptosis Analysis[2]

Cell Line: Mer-positive (Kasumi-1, NOMO-1) and Flt3-ITD (MV4;11, MOLM-13) AML cell lines
Concentration: 10, 25, 50, 100, 300nM
Incubation Time: 72 h
Result: Induced apoptosis in 50-67% of Mer-positive cells at 100 nM, and 68-76% of Mer-positive cells at 300 nM, with Kasumi-1 cells showing 76% apoptotic/dead cells at 300 nM.
Induced apoptosis in 54-67% of Flt3-ITD cells at 50 nM, and 90-98% of Flt3-ITD cells at 300 nM, with MV4;11 cells showing 90% apoptotic/dead cells at 300 nM and MOLM-13 cells showing 98% apoptotic/dead cells at 300 nM.
Confirmed increased cleavage of PARP and Caspase-3 in a dose-dependent manner via immunoblot.

Cell Proliferation Assay[2]

Cell Line: Mer-positive (Kasumi-1) and Flt3-ITD (MV4;11) AML cell lines
Concentration: 50, 100, 300nM
Incubation Time: 72 h (initial treatment)
Result: Resulted in only a 2.5-fold increase in viable cell number over 6 days in Kasumi-1 cells at 100 nM, compared to a 14-fold increase with vehicle.
Resulted in only a 13-fold increase in viable cell number over 6 days in MV4;11 cells at 50 nM, compared to a 67-fold increase with vehicle.
Caused more striking proliferation defects at higher concentrations, with minimal viable cells at Day 6.

Cell Proliferation Assay[2]

Cell Line: Mer-positive (Kasumi-1, NOMO-1) and Flt3-ITD (MV4;11, MOLM-13) AML cell lines
Concentration: 10, 25, 50, 100, 300nM
Incubation Time: Continuous treatment, medium renewed twice weekly (14-21 days total)
Result: Reduced Kasumi-1 cell colony formation by 90% at 100 nM.
Reduced NOMO-1 cell colony formation by 71% at 100 nM.
Reduced MV4;11 cell colony formation by 61% at 50 nM.
Reduced MOLM-13 cell colony formation by 93% at 50 nM.
Molecular Weight

513.66

Formula

C26H35N5O4S
CAS No.
SMILES

N(CCCC)C=1N=C2C(C(=CN2[C@H]3CC[C@H](O)CC3)C4=CC=C(S(=O)(=O)N5CCOCC5)C=C4)=CN1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

UNC1666 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UNC16661429882-12-1UNC 1666UNC-1666FLT3ERKAktSTATApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Extracellular signal regulated kinasesPKBProtein kinase Bdual-target Mer/Flt3 tyrosine kinase inhibitorprimary AMLKasumi-1 AML cellsMV4;11 Flt3-ITD AML cellsacute myeloid leukemiaInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
UNC1666
Cat. No.:
HY-120089
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.