1. Protein Tyrosine Kinase/RTK
    Apoptosis
  2. Ack1
    Anaplastic lymphoma kinase (ALK)
    Apoptosis
  3. KRCA-0008

KRCA-0008 

Cat. No.: HY-12331 Purity: 98.88%
COA Handling Instructions

KRCA-0008 is a selective ALK/Ack1 inhibitor with IC50s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer.

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

KRCA-0008 Chemical Structure

KRCA-0008 Chemical Structure

CAS No. : 1472795-20-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 67 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 67 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 86 In-stock
Estimated Time of Arrival: December 31
25 mg USD 158 In-stock
Estimated Time of Arrival: December 31
50 mg USD 310 In-stock
Estimated Time of Arrival: December 31
100 mg USD 527 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE KRCA-0008

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

KRCA-0008 is a selective ALK/Ack1 inhibitor with IC50s of 12 and 4 nM for ALK and Ack1, respectively. KRCA-0008 can be used for the research of cancer[1][2].

IC50 & Target

IC50: 12 nM (ALK), 4 nM (Ack1)[1]

In Vitro

KRCA-0008 (0-1000 μM) shows potency to ALK (wt), ALK L1196 M, ALK C1156Y, ALK F1174L, ALK R1275Q and insulin receptor with IC50s of 12, 75, 4, 17, 17 and 210 nM, respectively[1].
KRCA-0008 (0-1000 nM; 4 h) inhibits ALK-dependent signaling pathways more potently than crizotinib[2].
KRCA-0008 (0-1000 nM; 72 h) induces cell apoptosis[2].
KRCA-0008 (0-100 nM; 48 h) affects cell cycle[2].

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

Cell Proliferation Assay[1]

Cell Line: H3122 and H1993 cell lines
Concentration: 200 nM
Incubation Time: 6 hours
Result: Inhibited cell proliferation of H3122 and H1993 cells with IC50s of 0.08 and 3.6 nM, respectively.

Cell Proliferation Assay[2]

Cell Line: NPM-ALK-positive ALCL cell lines (Karpas-299 and SU-DHL-1) and U937 NPM ALK-negative lymphoma cell line
Concentration: 200 nM
Incubation Time: 72 hours
Result: Inhibited proliferation of Karpas-299, SU-DHL-1 and U937 cells with GI50s of 12 nM, 3 nM and 3.5 μM, respectively.

Western Blot Analysis[2]

Cell Line: Karpas-299 and SU-DHL-1 cell lines
Concentration: 0, 10, 100 and 1000 nM
Incubation Time: 4 hours
Result: Completely suppressed phosphorylation of ALK and its effectors at a dose of 100 nM in NPM-ALK-positive ALCL cells.

Apoptosis Analysis[2]

Cell Line: SU-DHL-1 cell line
Concentration: 0-1 μM
Incubation Time: 72 hours
Result: Dose-dependently increased cspase-3/7 activities and induced cell apoptosis.

Cell Cycle Analysis[2]

Cell Line: Karpas-299 and SU-DHL-1 cell lines
Concentration: 0-100 nM
Incubation Time: 48 hours
Result: Induced G0/G1 cell cycle arrest in ALCL cells expressing NPM-ALK.
In Vivo

KRCA-0008 (25 and 50 mg/kg; p.o. twice a day for two weeks) suppresses tumor growth in an ALK-positive Karpas-299 xenograft model[2].

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

Animal Model: NOD/SCID mice with Karpas-299 xenografts[2]
Dosage: 25 and 50 mg/kg
Administration: Oral gavage; 25 and 50 mg/kg twice a day; for two weeks
Result: Significantly inhibited tumor growth by inhibiting NPM-ALK phosphorylation without showing overt signs of toxicity or significant compound-related body weight loss.
Molecular Weight

609.12

Formula

C30H37ClN8O4

CAS No.
SMILES

ClC1=CN=C(NC2=CC=C(N3CCN(C(C)=O)CC3)C=C2OC)N=C1NC4=CC=C(N5CCN(C(C)=O)CC5)C=C4OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 230 mg/mL (377.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6417 mL 8.2086 mL 16.4171 mL
5 mM 0.3283 mL 1.6417 mL 3.2834 mL
10 mM 0.1642 mL 0.8209 mL 1.6417 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5.75 mg/mL (9.44 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5.75 mg/mL (9.44 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (2.05 mM); Clear solution

*All of the co-solvents are available by MCE.
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.
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.

  • 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

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
KRCA-0008
Cat. No.:
HY-12331
Quantity:
MCE Japan Authorized Agent: