| CAT # | Product Name | Tsanangudzo |
| CPD100501 | UNC2541 | UNC2541 ine simba uye MerTK-specific inhibitor inoratidza sub-micromolar inhibitory chiitiko musero-based ELISA. Mukuwedzera, chimiro che X-ray cheprotein yeMerTK yakaoma ne11 yakagadziriswa kuratidza kuti macrocycles aya anosunga muhomwe yeMerTK ATP. UNC2541 yakaratidza IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 inoveli pan-tam inhibitor, ichivharira iyo interface pakati pe tam ig1 ectodomain uye gas6 lg domain, zvine simba inhibiting axl reporter cell mitsara uye yekuzvarwa tam receptors cancer cell mitsara. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, inozivikanwawo seDE-120, inhibitor yeVEGF uye PDGF inogona kurapwa kwekunyorova kwakabatana nezera remacular degeneration. |
| CPD100742 | SGI-7079 | SGI-7079 ine simba uye inosarudza Axl inhibitor ine inogona kuita anticancer chiitiko. SGI-7079 yakanyatso kuvharidzira Axl activation pamberi peiyo exogenous Gas6 ligand. SGI-7079 inhibited bundu kukura mune dosi inotsamira nzira. Axl ndiyo inogona kurapa chinangwa chekukunda EGFR inhibitor kuramba. |
| CPD100741 | 2-D08 | 2-D08 iflavone yakagadzirwa inodzivirira sumoylation. 2-D08 yakaratidza anti-aggregatory uye neuroprotective effect |
| CPD100740 | Dubematinib | Dubermatinib, inozivikanwawo seTP-0903, ine simba uye inosarudza AXL inhibitor. TP-0903 induces apoptosis yakakura muCLL B masero ane LD50 kukosha kwenanomolar range. Musanganiswa weTP-0903 neBTK inhibitors inowedzera CLL B-cell apoptosis AXL overexpression inyaya inodzokororwa inocherechedzwa mumhando dzakawanda dzebundu dzakawana kuramba kune vakasiyana vamiririri. Kurapwa kwemaseru egomarara neTP-0903 kunodzosera mesenchymal phenotype mumamodhi akawanda uye kunosimudzira maseru egomarara kuti arapwe nevamwe vamiririri vakanangwa. Kutungamirirwa kweTP-0903 kungave semumiririri mumwe chete kana kusanganiswa neBTK inhibitors kunogona kushanda mukurapa varwere vane CLL. |
| CPD100739 | NPS-1034 | NPS-1034 ibhuku reMET inhibitor, iyo inhibita iyo yakagadziriswa MET receptor uye yayo inogadzirisa inoshanda shanduko. NPS-1034, inhibits akasiyana siyana anoshanda mutant mafomu eMET pamwe neHGF-activated wild-type MET. NPS-1034 yakadzivisa kuwanda kwemasero anoratidza yakabatidzwa MET uye akakurudzira kudzoreredzwa kwemamota akaumbwa kubva mumasero akadaro mune mbeva xenograft modhi kuburikidza neanti-angiogenic uye pro-apoptotic zviito. NPS-1034 zvakare yakavharira HGF-inosimudzira activation yeMET kusaina muhupo kana kusavapo kweserum. Zvinoshamisa, NPS-1034 yakavharira matatu MET akasiyana ayo anopokana neMET inhibitors SU11274, NVP-BVU972, uye PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, inozivikanwawo seMGCD-265, ndeyemuromo bioavailable, diki-morekuru, multitargeted tyrosine kinase inhibitor ine inogona kuita antineoplastic chiitiko. MGCD265 inosunga uye inhibits phosphorylation yeakawanda receptor tyrosine kinases (RTKs), kusanganisira c-Met receptor (hepatocyte growth factor receptor); iyo Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) marudzi 1, 2, uye 3; uye macrophage-inokurudzira 1 receptor (MST1R kana RON). |
| CPD100737 | CEP-40783 | CEP-40783, inozivikanwawo seRXDX-106, ine simba, inosarudza uye inowanikwa nemuromo inhibitor yeAXL uye c-Met ine IC50 tsika dze7 nM uye 12 nM, zvichiteerana kuti ishandiswe muzamu, isiri-diki cell lung (NSCLC) , uye pancreatic cancers. |
| CPD1725 | Bemcentinib | BGB-324, inozivikanwawo seR428 kana Bemcentinib, inosarudza diki molecule inhibitor yeAxl kinase, iyo yakaratidza chiitiko chekuvhara bundu kupararira uye kurebesa kurarama mumhando dzekenza yemazamu yemazamu. Iyo receptor tyrosine kinase Axl inogona kuita basa rakakosha mukufambira mberi kwegomarara, kupinda, metastasis, kuramba zvinodhaka, uye kufa kwemurwere. R428 inhibits Axl ine yakaderera nanomolar chiitiko uye yakavharira Axl-inotsamira zviitiko, zvinosanganisira Akt phosphorylation, kenza yemazamu cell invasion, uye proinflammatory cytokine kugadzirwa. |
| CPD3545 | Gilteritinib | Gilteritinib, inozivikanwawo seASP2215, ine simba FLT3/AXL inhibitor, yakaratidza zvine simba antileukemic chiitiko kurwisa AML pamwe kana zvese FLT3-ITD uye FLT3-D835 shanduko. Invitro, pakati pe78 tyrosine kinases yakaedzwa, ASP2215 inhibited FLT3, LTK, ALK, uye AXL kinases nepamusoro pe50% pa1 nM ine IC50 kukosha kwe0.29 nM yeFLT3, inenge 800-yakapetwa simba pane c-KIT, iyo inhibition iyo inobatanidzwa kune inogona kuitika ye myelosuppression. ASP2215 yakadzivisa kukura kwemasero eMV4-11, ayo ane FLT3-ITD, ane IC50 kukosha kwe0.92 nM, inoperekedzwa nekudzivisa pFLT3, pAKT, pSTAT5, pERK, uye pS6. ASP2215 yakadzikisa kuremerwa kwebundu mumwongo uye yakawedzera kurarama kwemakonzo akaiswa mutsinga neMV4-11 maseru. ASP2215 inogona kuve nekushandisa mukurapa AML. |
| CPD100734 | UNC2881 | UNC2881 ine simba Mer kinase inhibitor. UNC2281 inhibits steady-state Mer kinase phosphorylation ine IC50 kukosha kwe22 nM. Kurapa neUNC2281 kunokwanawo kuvhara EGF-mediated stimulation ye chimeric receptor ine intracellular domain yeMer fused kune extracellular domain yeEGFR. Pamusoro pezvo, UNC2881 inovharisa zvine simba collagen-induced platelet aggregation, zvichiratidza kuti iyi kirasi yeinhibitors inogona kuve nerubatsiro rwekudzivirira uye/kana kurapwa kwepathologic thrombosis. |
| CPD100733 | UNC2250 | UNC2250 ine simba uye inosarudza Mer Kinase inhibitor. Kana yakashandiswa kune masero mhenyu, UNC2250 inhibited steady-state phosphorylation ye endogenous Mer ine IC50 ye9.8 nM uye yakavhara ligand-yakakurudzira kushandiswa kwechimeric EGFR-Mer protein. Kurapwa neUNC2250 kwakakonzerawo kudzikira kwekoloni-kuumba mukana muRhabdoid uye NSCLC tumor cell, zvichiratidza kushanda kweantitumor chiitiko. Mhedzisiro yacho inopa chikonzero chekuwedzera kuferefetwa kweUNC2250 yekurapa kwekushandisa muvarwere vane cancer. |
| CPD100732 | LDC1267 | LDC1267 ine simba uye inosarudza TAM kinase inhibitor. LDC1267 inoratidza yakaderera chiitiko ichipokana neMet, Aurora B, Lck, Src, uye CDK8. LDC1267 yakaderedza zvakanyanya murine mammary cancer uye melanoma metastases zvinoenderana neNK masero. Iyo TAM tyrosine kinase receptors Tyro3, Axl uye Mer (inozivikanwawo seMertk) yakaonekwa seubiquitylation substrates yeCbl-b. Kurapwa kwemusango-mhando NK masero ane achangogadzirwa molecule diki TAM kinase inhibitor inopa kurapa kugona, zvinobudirira kusimudzira anti-metastatic NK cell chiitiko mu vivo. |
| CPD100731 | BMS-777607 | BMS-777607, inozivikanwawo seBMS-817378 uye ASLAN-002, Met tyrosine kinase inhibitor, inhibitor yeMET tyrosine kinase ine inogona kuita antineoplastic chiitiko. MET tyrosine kinase inhibitor BMS-777607 inosunga ku-c-Met protein, kana hepatocyte growth factor receptor (HGFR), kudzivirira kusungirirwa kwehepatocyte growth factor (HGF) uye kuvhiringidza nzira yekuratidzira yeMET; mumiririri uyu anogona kukonzera kufa kwesero mumabundu maseru anoratidza c-Met. c-Met, receptor tyrosine kinase yakanyanyisa kana yakashandurwa mumhando dzakawanda dzebundu masero, inoita basa rakakosha mukuwanda kwebundu masero, kupona, kupinda, uye metastasis, uye mubundu angiogenesis. |
| CPD100730 | Cabozantinib | Cabozantinib, inozivikanwawo seXL-184 kana BMS-907351, ndeyemuromo bioavailable, diki molecule receptor tyrosine kinase (RTK) inhibitor ine inogona kuita antineoplastic chiitiko. Cabozantinib inosunga zvakasimba uye inodzivisa akati wandei tyrosine receptor kinases. Kunyanya, cabozantinib inoratidzika kuva nehukama hwakasimba hwehepatocyte growth factor receptor (Met) uye vascular endothelial growth factor receptor 2 (VEGFR2), iyo inogona kuguma nekudzivisa kukura kwebundu uye angiogenesis, uye kudzoka kwebundu. Cabozantinib yakabvumidzwa neUS FDA muna Mbudzi 2012 kurapwa kwemedullary thyroid cancer. |
