IHMT-TRK-284 

IHMT-TRK-284 (Compound 34) is a potent, orally active type II TRK kinase inhibitor with IC₅₀ values of 10.5, 0.7, and 2.6 nM to TRKA, B, and C respectively. IHMT-TRK-284 displays great selectivity profile in the kinome and good in vivo antitumor efficacies^[1].

IHMT-TRK-284 (Compound 34) (0-10 µM, 72 h) shows antiproliferative effects against BaF3 cells, a panel of kinase transformed BaF3 cells, and KM-12-LUC cells^[1].
IHMT-TRK-284 (0-10 µM, 24 h) induces apoptosis and arrests the cell cycle into G0/G1 phase in KM-12-LUC cells^[1].
IHMT-TRK-284 exerts its inhibitory effect to the colon cancer cells through on-target inhibition of TRK^[1].
IHMT-TRK-284 could overcome drug resistant mutants including V573M and F589L in the ATP binding pocket as well as G667C/S in the DFG region^[1].
IHMT-TRK-284 shows selectivity over VEGFR2 kinase^[1].

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

IHMT-TRK-284 (Compound 34) (40 and 80 mg/kg; p.o.; daily, 10 days) shows good in vivo PK and antitumor efficacy properties^[1].

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

Animal Model:	Four-week old female nu/nu mice, one million BaF3-TELTRKA, BaF3-TEL-TRKB, BaF3-TEL-TRKC, BaF3-LMNA-TRKA-F589L, BaF3-LMNA-TRKA-G667S, and five million KM-12-LUC cells in DMEM medium were formulated as a 1:1 mixture with matrigel and injected into the subcutaneous space on the right flank of nu/nu mice[1]
Dosage:	40 mg/kg and 80 mg/kg
Administration:	Daily oral gavage, 10 days
Result:	Dose-dependently inhibited the BaF3-TEL-TRKA, BaF3-TEL-TRKB, and BaF3-TEL-TRKC tumor progression with TGI (tumor growth inhibition) of 68%, 93%, and 58%. Dose-dependently inhibited the tumor progression and exhibited the TGI of 93% at 40 mg/kg/day and 95% at 80 mg/kg/day in KM-12-LUC cells inoculated xenograft mouse model. Potently inhibited the tumor growth with TGI values of 88% and 89% respectively at 80 mg/kg dosage in BaF3- LMNA-TRKA-F589L and BaF3-LMNA-TRKA-G667S cells.

Animal Model:	Mice, sprague dawley rats, and beagle dogs[1]
Dosage:	1 mg/kg and 10 mg/kg
Administration:	Intravenous injection and oral administration (Pharmacokinetic Analysis)
Result:	Pharmacokinetic study of IHMT-TRK-284 in mice, sprague dawley rats, and beagle dogsa[1] Parameter Mice i.v. (1 mg/kg) Mice p.o. (10 mg/kg) Rats i.v. (1 mg/kg) Rats p.o. (10 mg/kg) Beagle Dogs i.v. (1 mg/kg) Beagle Dogs p.o. (10 mg/kg) AUC(0-t) (ng/mL*h) 748 1431 393 952 323 464 Tmax (h) 0.033 1.5 0.03 4.7 0.08 4.3 T1/2 (h) 2.6 3.4 2.7 2.5 0.03 11.8 Vz (mL/kg) 4934 31567 9682 Molecular Weight 473.59 Formula C25H27N7OS CAS No. 2416844-79-4 SMILES O=C(NC1=NC(C)=C(C2=CC3=C(C=C2)C(/C=C/C4=NC=CC=C4)=NN3)S1)CN5CCN(C)CC5 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 Data Sheet (282 KB) Handling Instructions (2659 KB) References [1]. Beilei Wang, et al. Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistan  [Content Brief] [1]. Beilei Wang, et al. Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistan Rating Lot Number * Submit an Image No file chosen (Maximum size is: 1024 Kb) PubMed ID If you have published this work, please enter the PubMed ID. Show My Name Your name will appear on the site. Email Remarks IHMT-TRK-284 Related Classifications Neuronal Signaling Protein Tyrosine Kinase/RTK Apoptosis Trk Receptor c-Fms PDGFR Bcr-Abl c-Kit Apoptosis Molarity Calculator Dilution Calculator The molarity calculator equation Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Mass   Concentration   Volume   Molecular Weight * kg g mg μg ng pg = M mM μM nM pM × L mL μL × 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) M mM μM nM pM × L mL μL = M mM μM nM pM × L mL μL 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: IHMT-TRK-2842416844-79-4Trk Receptorc-FmsPDGFRBcr-Ablc-KitApoptosisTropomyosin related kinase receptor CSF-1 receptorcolony stimulating factor 1 receptorCSF-1RCSF1RPlatelet-derived growth factor receptorSCFRCD117SelectivityAntitumorBaF3KM-12-LUCInhibitorinhibitorinhibit Your Recently Viewed Products: Inquiry Online Your information is safe with us. * Required Fields. Product Name   Salutation Dr. Prof. Mr. Ms. Mrs. Miss. Applicant Name *   Email Address * Phone Number *   Organization Name * Department *   Requested quantity * mg g kg t ml l Country or Region * United StatesCanadaUnited KingdomAustraliaChinaGermanyFranceJapanKorea SouthSwitzerland------------------------------AlbaniaAlgeriaArgentinaArmeniaAustraliaAustriaAzerbaijanBahrainBangladeshBarbadosBelarusBelgiumBoliviaBosnia HerzegovinaBrazilBulgariaCameroonCanadaChileChinaColombiaCroatiaCyprusCzech RepublicDenmarkEcuadorEgyptEstoniaFijiFinlandFranceGeorgiaGermanyGibraltarGreeceHong Kong, ChinaHungaryIcelandIndiaIndonesiaIranIraqIrelandIsraelItalyJapanJordanKazakhstanKenyaKorea SouthKuwaitLatviaLebanonLibyaLithuaniaLuxembourgMacedoniaMalaysiaMaltaMexicoMoldovaMonacoMongoliaMontenegroMoroccoNepalNetherlandsNew ZealandNigeriaNorwayOmanPakistanParaguayPeruPhilippinesPolandPortugalPuerto RicoQatarRepublic of BeninRomaniaRussiaSaudi ArabiaSerbiaSingaporeSlovakiaSloveniaSouth AfricaSpainSri LankaSurinameSwedenSwitzerlandSyriaTaiwan, ChinaThailandTunisiaTurkeyUkraineUnited Arab EmiratesUnited KingdomUnited StatesUruguayUzbekistanVenezuelaVietnamZambiaZimbabweOther CountriesMacao, China       Please select a local distributor ナミキ商事株式会社 コスモ・バイオ株式会社 Remarks Bulk Inquiry Inquiry Information Product Name: IHMT-TRK-284 Cat. No.: HY-146697 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 * United StatesCanadaUnited KingdomAustraliaChinaGermanyFranceJapanKorea SouthSwitzerland------------------------------AlbaniaAlgeriaArgentinaArmeniaAustraliaAustriaAzerbaijanBahrainBangladeshBarbadosBelarusBelgiumBoliviaBosnia HerzegovinaBrazilBulgariaCameroonCanadaChileChinaColombiaCroatiaCyprusCzech RepublicDenmarkEcuadorEgyptEstoniaFijiFinlandFranceGeorgiaGermanyGibraltarGreeceHong Kong, ChinaHungaryIcelandIndiaIndonesiaIranIraqIrelandIsraelItalyJapanJordanKazakhstanKenyaKorea SouthKuwaitLatviaLebanonLibyaLithuaniaLuxembourgMacedoniaMalaysiaMaltaMexicoMoldovaMonacoMongoliaMontenegroMoroccoNepalNetherlandsNew ZealandNigeriaNorwayOmanPakistanParaguayPeruPhilippinesPolandPortugalPuerto RicoQatarRepublic of BeninRomaniaRussiaSaudi ArabiaSerbiaSingaporeSlovakiaSloveniaSouth AfricaSpainSri LankaSurinameSwedenSwitzerlandSyriaTaiwan, ChinaThailandTunisiaTurkeyUkraineUnited Arab EmiratesUnited KingdomUnited StatesUruguayUzbekistanVenezuelaVietnamZambiaZimbabweOther CountriesMacao, China Remarks Request for HNMR Report We have received your request and will respond to you as soon as possible. [email protected] 609-228-6898 Find Your Local Distributor MedChemExpress Contact Us About Us Headquarters Distributors Statement on False Report Careers Customer Support Technical Support Service Ordering Information Easy Return Shipping Rates & Policies Intellectual Property Promise Resources Free Sample Resources Molarity Calculator Dilution Calculator Terms & Conditions Reconstitution Calculator Specific Activity Calculator Subscribe to our E-newsletter Name Email * Sorry, but the email address you supplied was invalid. Thanks, your subscription has been confirmed. You will hear from us soon. Submission failed, please try again later. Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients. Copyright © 2013-2024 MedChemExpress. All Rights Reserved. Site Map Privacy Policy Join with us As the situation with COVID-19 continues to unfold in every community, MedChemExpress (MCE) is responding to the uncertainty caused by this outbreak thoughtfully and cautiously. Your need for high quality reagent doesn't stop during difficult times, and neither do we. We're doing our best to keep everyone healthy and safe in the workplace while also avoiding the interruptions to our day-to-day operations. If you need to change the delivery plan for items ordered, please contact us via email [email protected]. Thank you for being a loyal MedChemExpress (MCE) customer, we are here to assist you as needed.