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

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  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 67 In-stock
Solution
10 mM * 1 mL in DMSO USD 67 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 70 In-stock
25 mg USD 140 In-stock
50 mg USD 240 In-stock
100 mg USD 400 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

KRCA-0008 Related Antibodies

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].

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

KRCA-0008 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to gray

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 5.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (57.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6417 mL 8.2086 mL 16.4171 mL 41.0428 mL
5 mM 0.3283 mL 1.6417 mL 3.2834 mL 8.2086 mL
10 mM 0.1642 mL 0.8209 mL 1.6417 mL 4.1043 mL
15 mM 0.1094 mL 0.5472 mL 1.0945 mL 2.7362 mL
20 mM 0.0821 mL 0.4104 mL 0.8209 mL 2.0521 mL
25 mM 0.0657 mL 0.3283 mL 0.6567 mL 1.6417 mL
30 mM 0.0547 mL 0.2736 mL 0.5472 mL 1.3681 mL
40 mM 0.0410 mL 0.2052 mL 0.4104 mL 1.0261 mL
50 mM 0.0328 mL 0.1642 mL 0.3283 mL 0.8209 mL
60 mM 0.0274 mL 0.1368 mL 0.2736 mL 0.6840 mL
80 mM 0.0205 mL 0.1026 mL 0.2052 mL 0.5130 mL
100 mM 0.0164 mL 0.0821 mL 0.1642 mL 0.4104 mL
  • 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.

KRCA-0008 Related Classifications

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:

KRCA-00081472795-20-2KRCA0008KRCA 0008Ack1Anaplastic lymphoma kinase (ALK)ApoptosisActivated Cdc42 kinase 1TNK2Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246N-AcetylpiperidinediaminopyrimidineselectiveanaloguecrizotinibALCLapoptosiscell cycle arrestInhibitorinhibitorinhibit

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:

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)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB)

Request for HNMR Report

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