연구용
제품 번호S1119
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| E98NT | Growth Inhibition Assay | 0.01-10 μM | DMSO | IC50=89 nM | 23484006 | |
| SNU-5 | Growth Inhibition Assay | IC50= 19 nM | 21926191 | |||
| Hs746T | Growth Inhibition Assay | IC50=9.9 nM | 21926191 | |||
| SNU-1 | Growth Inhibition Assay | IC50=5223 nM | 21926191 | |||
| SNU-16 | Growth Inhibition Assay | IC50=1149 nM | 21926191 | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50= 6421 nM | 21926191 | |||
| U87MG | Growth Inhibition Assay | IC50=1851 nM | 21926191 | |||
| H441 | Growth Inhibition Assay | IC50=21700 nM | 21926191 | |||
| H69 | Growth Inhibition Assay | IC50=20200 nM | 21926191 | |||
| PC3 | Growth Inhibition Assay | IC50=10800 nM | 21926191 | |||
| MTC-TT | Growth Inhibition Assay | IC50=0.04 + 0.03 μM | 21470995 | |||
| MZ-CRC | Growth Inhibition Assay | IC50> 5 μM | 21470995 | |||
| TPC-1 | Growth Inhibition Assay | IC50=0.06 + 0.02 μM | 21470995 | |||
| NIH-3T3/TPR-Met | Function assay | Inhibition of cell proliferation in mouse NIH-3T3/TPR-Met cells, IC50 = 1 μM. | 24996144 | |||
| BA/F3 | Growth inhibition assay | Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition, GI50 = 0.003 μM. | 26652860 | |||
| BaF3 | Growth inhibition assay | 48 hrs | Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.01 μM. | 26652860 | ||
| BA/F3 | Growth inhibition assay | 48 hrs | Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.05 μM. | 26652860 | ||
| TT | Growth inhibition assay | 10 days | Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay, GI50 = 0.12 μM. | 26652860 | ||
| BA/F3 | Growth inhibition assay | 48 hrs | Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.89 μM. | 26652860 | ||
| BaF3 | Growth inhibition assay | 48 hrs | Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.91 μM. | 26652860 | ||
| Nthy-ori 3-1 | Cytotoxicity assay | 10 days | Cytotoxicity against human Nthy-ori 3-1 cells after 10 days by MTT assay, GI50 = 4.93 μM. | 26652860 | ||
| BAF3 | Function assay | 0.01 to 10 uM | 1 hr | Inhibition of TEL-fused wild type Ret (unknown origin) phosphorylation at Y1062/Y905 expressed in mouse BAF3 cells at 0.01 to 10 uM after 1 hr by Western blot analysis | 26652860 | |
| TT | Function assay | 4 hrs | Inhibition of autophosphorylation of RET C634W mutant at Y905 in human TT cells at 1 uM after 4 hrs by Western blot analysis | 26652860 | ||
| BAF3 | Function assay | 0.01 to 10 uM | 1 hr | Inhibition of TEL-fused Ret S891A mutant (unknown origin) phosphorylation at Y1062/Y905 expressed in mouse BAF3 cells at 0.01 to 10 uM after 1 hr by Western blot analysis | 26652860 | |
| BAF3 | Function assay | 0.01 to 10 uM | 1 hr | Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BAF3 cells assessed as suppression of phosphorylation of PLCgamma at Y783 at 0.01 to 10 uM after 1 hr by Western blot analysis | 26652860 | |
| BAF3 | Function assay | 0.01 to 10 uM | 1 hr | Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BAF3 cells assessed as suppression of phosphorylation of Shc at Y317 at 0.01 to 10 uM after 1 hr by Western blot analysis | 26652860 | |
| TT | Function assay | 1 to 10 uM | 4 hrs | Inhibition of RET C634W mutant in human TT cells assessed as suppression of PLCgamma phosphorylation at Y783 at 1 to 10 uM after 4 hrs by Western blot analysis | 26652860 | |
| TT | Function assay | 1 to 10 uM | 4 hrs | Inhibition of RET C634W mutant in human TT cells assessed as suppression of ERK phosphorylation at T202/Y204 at 1 to 10 uM after 4 hrs by Western blot analysis | 26652860 | |
| TT | Function assay | 1 to 10 uM | 4 hrs | Inhibition of RET C634W mutant in human TT cells assessed as suppression of AKT phosphorylation at T308/S473 at 1 to 10 uM after 4 hrs by Western blot analysis | 26652860 | |
| TT | Function assay | 1 uM | Inhibition of Ret-driven oncogenic transformation of human TT cells at 1 uM by soft agar assay | 26652860 | ||
| TT | Function assay | 1 uM | 4 hrs | Inhibition of autophosphorylation of RET C634W mutant at Y1062 in human TT cells at 1 uM after 4 hrs by Western blot analysis | 26652860 | |
| TT | Apoptosis assay | 1 uM | 96 hrs | Induction of apoptosis in human TT cells expressing Ret C634W mutant at 1 uM after 96 hrs by annexinV/PI staining-based flow cytometric analysis | 26652860 | |
| PC3 | Function assay | 1 to 3 hrs | Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs, IC50 = 1.9 μM. | 26717201 | ||
| MDA-MB-231 | Function assay | 1 to 3 hrs | Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs, IC50 = 5 μM. | 26717201 | ||
| BAF3 | Function assay | 1 to 3 hrs | Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs, IC50 = 7.5 μM. | 26717201 | ||
| MDA-MB-231 | Function assay | 1 to 3 hrs | Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs, IC50 = 42 μM. | 26717201 | ||
| BA/F3 | Function assay | 48 hrs | Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.014 μM. | 26874741 | ||
| Sf21 | Function assay | 15 mins | Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay, IC50 = 0.016 μM. | 26874741 | ||
| BA/F3 | Function assay | 48 hrs | Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.19 μM. | 26874741 | ||
| BA/F3 | Function assay | 48 hrs | Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.19 μM. | 26874741 | ||
| BA/F3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay, IC50 = 0.0219 μM. | 27068889 | ||
| Sf21 | Function assay | 60 mins | Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA, IC50 = 0.003 μM. | 27131066 | ||
| Sf21 | Function assay | 60 mins | Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA, IC50 = 0.811 μM. | 27131066 | ||
| BaF3 | Function assay | 72 hrs | Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay, IC50 = 0.889 μM. | 27131066 | ||
| BaF3 | Function assay | 72 hrs | Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay, IC50 = 0.889 μM. | 27131066 | ||
| Ba/F3 | Function assay | Inhibition of RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.07 μM. | 27814560 | |||
| TT | Function assay | Inhibition of RET C634W mutant in human TT cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.26 μM. | 27814560 | |||
| Ba/F3 | Function assay | Inhibition of RET V804M mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.74 μM. | 27814560 | |||
| Nthy-ori 3-1 | Cytotoxicity assay | Cytotoxicity against human Nthy-ori 3-1 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 2.92 μM. | 27814560 | |||
| HepG2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 0.012 μM. | 28412159 | ||
| EBC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0514 μM. | 28412159 | ||
| H1299 | Growth inhibition assay | 72 hrs | Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay, IC50 = 1.919 μM. | 28651979 | ||
| MCF7 | Growth inhibition assay | 72 hrs | Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay, IC50 = 2.889 μM. | 28651979 | ||
| A549 | Growth inhibition assay | 72 hrs | Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay, IC50 = 4.205 μM. | 28651979 | ||
| T47D | Growth inhibition assay | 72 hrs | Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay, IC50 = 4.448 μM. | 28651979 | ||
| H460 | Growth inhibition assay | 72 hrs | Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay, IC50 = 5.669 μM. | 28651979 | ||
| HuH7 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 4.348 μM. | 29057042 | ||
| A498 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 8.456 μM. | 29057042 | ||
| NCI-H727 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay, IC50 = 14.01 μM. | 29057042 | ||
| BAF3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against mouse BAF3 cells harboring TRP-MET after 72 hrs by CCK-8 assay, IC50 = 0.024 μM. | 29146452 | ||
| A549 | Cytotoxicity assay | 10 uM | 72 hrs | Cytotoxicity against human A549 cells at 10 uM after 72 hrs by Incucyte live-cell imaging analysis | 29407963 | |
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | |||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | |||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | |||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | |||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | |||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | |||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | |||
| EBC1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0048 μM. | 30248654 | ||
| MKN45 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.0069 μM. | 30248654 | ||
| SNU5 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay, IC50 = 0.0121 μM. | 30248654 | ||
| BAF3 | Function assay | 72 hrs | Inhibition of TPR-tagged met (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.01986 μM. | 30248654 | ||
| NCI-H460 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.0401 μM. | 30248654 | ||
| MGHU3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MGHU3 cells after 72 hrs by CellTiter-Glo assay | 30309671 | ||
| RT112 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay | 30309671 | ||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 501.51 | 화학식 | C28H24FN3O5 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 849217-68-1 | SDF 다운로드 | 원액 보관 |
|
|
| 동의어 | BMS-907351 | Smiles | COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F | ||
|
In vitro |
DMSO
: 100 mg/mL
(199.39 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)
2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)
계산 결과:
작업 농도: mg/ml;
DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.
생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.
참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.
| Targets/IC50/Ki |
VEGFR2/KDR
(Cell-free assay) 0.035 nM
c-Met
(Cell-free assay) 1.3 nM
Axl
(Cell-free assay) 7 nM
|
|---|---|
| 시험관 내(In vitro) |
Cabozantinib (XL184)는 RON 및 PDGFRβ에 대해 각각 124 nM 및 234 nM의 IC50로 약한 억제 활성을 가지며, FGFR1에 대해 5.294 μM의 IC50로 낮은 활성을 가집니다. 낮은 농도 (0.1-0.5 μM)에서, 이는 MPNST 세포에서 구성적 및 유도성 Met 인산화 및 그 결과로 나타나는 하류 신호 전달의 현저한 억제를 유도하고, HGF 유도 MPNST 세포 이동 및 침윤을 억제하기에 충분합니다. 이 화합물은 또한 사이토카인 자극된 인간 제대정맥 내피 세포 (HUVEC)에서 Met 및 VEGFR2 인산화의 현저한 억제를 유도합니다. 0.1 μM에서 MPNST 세포 성장에 유의미한 영향을 미치지 않지만, 5-10 μM의 XL184는 MPNST 세포 성장을 유의미하게 억제합니다.
|
| 생체 내(In vivo) |
자발적 췌장 소도 종양을 가진 RIP-Tag2 마우스에서 30 mg/kg의 Cabozantinib (XL184) 치료는 종양 혈관 형성의 83%를 방해하고, 주변 세포 및 비어있는 기저막 슬리브를 감소시키며, 광범위한 종양 내 저산소증 및 광범위한 종양 세포 apoptosis를 유발하고, 약물 중단 후 종양 혈관 형성의 재성장을 늦춥니다. VEGFR은 차단하지만 c-Met은 차단하지 않는 XL999와 비교하여 혈관성이 43%만 감소하는 것보다 훨씬 더 유의미하게, 이는 VEGFR 및 기타 기능적으로 관련 있는 수용체 티로신 키나아제 (RTK)의 동시 억제가 혈관 형성 억제를 증폭시킨다는 것을 시사합니다. 이 화합물은 또한 원발성 종양의 침습성을 감소시키고 전이를 줄입니다. 30 mg/kg/일에서, 이는 SCID 마우스에서 인간 MPNST 이종 이식편의 성장 및 전이를 유의미하게 억제합니다. XL184의 투여는 유방, 폐 및 신경교종 종양 모델에서 용량 의존적으로 종양 성장을 억제하며, 이는 종양 및 내피 세포 증식 감소 및 apoptosis 증가와 관련이 있습니다. 단일 경구 투여는 MDA-MB-231 종양 보유 마우스 및 C6 종양 보유 쥐에서 각각 100 mg/kg 및 10 mg/kg에서 지속적인 종양 성장 억제를 유도하기에 충분합니다.
|
참조 |
|
| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | p-MET / p-ERK / p-AKT p-MET(Y1234/1235) / MET / p-EGFR(Y1068) / EGFR / p-Gab1(Y627) / Gab1 / p-AKT(S473) / p-ERK / p-EIF4E |
|
29520051 |
| Immunofluorescence | α-tubulin |
|
29520051 |
| Growth inhibition assay | Cell viability |
|
23661005 |
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT06156410 | Recruiting | Ewing Sarcoma|Osteosarcoma |
Children''s Hospital of Philadelphia|Children''s Hospital Colorado|Exelixis|Alex''s Lemonade Stand Foundation |
October 24 2023 | Phase 1 |
| NCT05249114 | Active not recruiting | Neuroendocrine Tumors |
Providence Health & Services|Exelixis|Advanced Accelerator Applications SA |
December 28 2022 | Phase 1 |
| NCT05444933 | Completed | Advanced Renal Cell Carcinoma |
Ipsen |
September 16 2022 | -- |