연구용
제품 번호S2853
| 세포주 | 분석 유형 | 농도 | 배양 시간 | 제형 | 활성 설명 | PMID |
|---|---|---|---|---|---|---|
| MM.1S | Growth Inhibition Assay | 0-100 nM | 48 h | IC50 = 10 nM | 25312543 | |
| NCI-H929 | Growth Inhibition Assay | 0-100 nM | 48 h | IC50 = 14 nM | 25312543 | |
| SUDHL16 | Apoptosis Asssay | 2.5–3.5 nM | 48 h | enhances the cell death co-treatment with ACY1215 | 25239935 | |
| SUDHL14 | Apoptosis Asssay | 2.5–3.5 nM | 48 h | enhances the cell death co-treatment with ACY1215 | 25239935 | |
| U2932 | Apoptosis Asssay | 2.5–3.5 nM | 48 h | enhances the cell death co-treatment with ACY1215 | 25239935 | |
| P-UMSCC-1 | Growth Inhibition Assay | IC50=11.2 nM | 24915039 | |||
| R-UMSCC-1 | Growth Inhibition Assay | IC50=2294 nM | 24915039 | |||
| P-Cal33 | Growth Inhibition Assay | IC50=17.3 nM | 24915039 | |||
| R-Cal33 | Growth Inhibition Assay | IC50=1112 nM | 24915039 | |||
| Jurkat | Growth Inhibition Assay | 1-11nM | 48 h | inhibits the cell proliferation co-treatment with vorinostat | 24801128 | |
| Jurkat | Apoptosis Asssay | 8 nM | 24/48 h | induces apoptosis, caspase activation, and PARP cleavage co-treatment with vorinostat | 24801128 | |
| UMSCC-22A | Apoptosis Asssay | 200 nM | 24 h | induce the cell apoptosis co-treatment with ONX 0912 | 22929803 | |
| UMSCC-22B | Apoptosis Asssay | 200 nM | 24 h | induce the cell apoptosis co-treatment with ONX 0912 | 22929803 | |
| 1483 | Apoptosis Asssay | 200 nM | 24 h | induce the cell apoptosis co-treatment with ONX 0912 | 22929803 | |
| UMSCC-1 | Apoptosis Asssay | 200 nM | 24 h | induce the cell apoptosis co-treatment with ONX 0912 | 22929803 | |
| UMSCC-22A | Growth Inhibition Assay | IC50=38.7 ± 1.0 nM | 22929803 | |||
| UMSCC-22B | Growth Inhibition Assay | IC50=30.7 ± 9.3 nM | 22929803 | |||
| 1483 | Growth Inhibition Assay | IC50=50.5 ± 11.9 nM | 22929803 | |||
| UMSCC-1 | Growth Inhibition Assay | IC50=34.6 ± 2.6 nM | 22929803 | |||
| Cal33 | Growth Inhibition Assay | IC50=49.3 ± 8.9 nM | 22929803 | |||
| PCI-15A | Growth Inhibition Assay | IC50=70.4 ± 22.6 nM | 22929803 | |||
| PCI-15B | Growth Inhibition Assay | IC50=39.5 ± 11.0 nM | 22929803 | |||
| OSC-19 | Growth Inhibition Assay | IC50=18.3 ± 4.2 nM | 22929803 | |||
| SUDHL16 | Apoptosis Asssay | 2.0-4.0 nM | 48 h | induces cell death co-treatment with obatoclax | 22411899 | |
| SUDHL16 | Function Assay | 2.5 nM | 24 h | activates JNK, inactivates AKT, up-regulates Noxa, and induces γH2A.X co-treatment with obatoclax | 22411899 | |
| Granta | Growth Inhibition Assay | 0-4 nM | 48 h | induce cell death co-treatment with HADCIs | 21750224 | |
| SUDHL16 | Growth Inhibition Assay | 1-4 nM | 36 h | induce cell death co-treatment with HADCIs | 20233973 | |
| MOLT4 | Function assay | 1 hr | Inhibition of chymotrypsin-like activity of 20S proteasome in human MOLT4 cells after 1 hr by CellTiter-Glo luminescent assay, IC50 = 0.0051 μM. | 19348473 | ||
| MESSA | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.018 μM. | 19348473 | ||
| MESSA | Cytotoxicity assay | 72 hrs | Cytotoxicity against multidrug resistance transporter expressing doxorubicin resistant human MESSA cells assessed as cell viability after 72 hrs by CellTiter-Glo luminescent assay, IC50 = 0.413 μM. | 19348473 | ||
| RPMI8226 | Cytotoxicity assay | 72 hrs | Cytotoxic activity against human RPMI8226 cells after 72 hrs by MTS assay, IC50 = 0.01319 μM. | 24767818 | ||
| NCI-H929 | Cytotoxicity assay | 72 hrs | Cytotoxic activity against human NCI-H929 cells after 72 hrs by MTS assay, IC50 = 0.02132 μM. | 24767818 | ||
| CCRF-CEM | Antiproliferative assay | 72 hrs | Antiproliferative activity against human CCRF-CEM cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0061 μM. | 26231162 | ||
| RPMI8266 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RPMI8266 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0139 μM. | 26231162 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0193 μM. | 26231162 | ||
| A431 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A431 cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM. | 26231162 | ||
| TOV21G | Antiproliferative assay | 72 hrs | Antiproliferative activity against human TOV21G cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0238 μM. | 26231162 | ||
| RKO | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RKO cells after 72 hrs by oxyluciferin luminescence assay, IC50 = 0.0271 μM. | 26231162 | ||
| MM1S | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM. | 27765408 | ||
| RPMI8226 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM. | 27765408 | ||
| LCL | Cytotoxicity assay | 48 hrs | Cytotoxicity against human LCL cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.03 μM. | 27994734 | ||
| RD-ES | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RD-ES cells harboring p53 mutant assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.043 μM. | 27994734 | ||
| U266 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human U266 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.06 μM. | 27994734 | ||
| WE68 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human WE68 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.08 μM. | 27994734 | ||
| IMR90 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human IMR90 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.13 μM. | 27994734 | ||
| MCF10A | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF10A cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM. | 27994734 | ||
| SKOV3 | Cytotoxicity assay | 48 hrs | Cytotoxicity against p53 deficient human SKOV3 cells assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.32 μM. | 27994734 | ||
| MDA-MB-468 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-468 cells harboring mutant p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.33 μM. | 27994734 | ||
| HNDF | Cytotoxicity assay | 48 hrs | Cytotoxicity against HNDF cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.35 μM. | 27994734 | ||
| KGN | Cytotoxicity assay | 48 hrs | Cytotoxicity against human KGN cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 0.45 μM. | 27994734 | ||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells harboring wild type p53 assessed as reduction in cell viability after 48 hrs by 7AAD-staining based FACS analysis, LD50 = 4.5 μM. | 27994734 | ||
| MCF7 | Function assay | 35 nM | 4 hrs | Inhibition of 26S proteasome in human MCF7 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis | 27994734 | |
| MDA-MB-468 | Function assay | 35 nM | 4 hrs | Inhibition of 26S proteasome in human MDA-MB-468 cells assessed as accumulation of high molecular weight polyubiquitin-conjugated proteins at 35 nM after 4 hrs by Western blot analysis | 27994734 | |
| MM1S | Cytotoxicity assay | 72 hrs | Cytotoxicity against human MM1S cells measured after 72 hrs by MTS assay, IC50 = 0.0015 μM. | 28027531 | ||
| RPMI8226 | Cytotoxicity assay | 72 hrs | Cytotoxicity against human RPMI8226 cells measured after 72 hrs by MTS assay, IC50 = 0.0132 μM. | 28027531 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | |||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | |||
| 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 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) 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 | |||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | |||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells | 29435139 | |||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 29435139 | |||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH 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 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 29435139 | |||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells | 29435139 | |||
| Rh30 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells | 29435139 | |||
| fibroblast cells | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast 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 | |||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells | 29435139 | |||
| Daoy | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 cells | 29435139 | |||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells | 29435139 | |||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) 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 | |||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC 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 | |||
| Rh18 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 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 | |||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells | 29435139 | |||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells | 29435139 | |||
| ANBL-6 | Function assay | Inhibition of 20S proteasome activity in human ANBL-6 cells, IC50 = 0.01 μM. | 29652143 | |||
| MCF7 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.0041 μM. | 30165344 | ||
| MDA-MB-231 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay, IC50 = 0.0044 μM. | 30165344 | ||
| RPMI8226 | Cytotoxicity assay | 48 hrs | Cytotoxicity against human RPMI8226 cells after 48 hrs by MTT assay, IC50 = 0.0067 μM. | 30165344 | ||
| 클릭하여 더 많은 세포주 실험 데이터 보기 | ||||||
| 분자량 | 719.91 | 화학식 | C40H57N5O7 |
보관 (수령일로부터) | |
|---|---|---|---|---|---|
| CAS 번호 | 868540-17-4 | SDF 다운로드 | 원액 보관 |
|
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| 동의어 | N/A | Smiles | CC(C)CC(C(=O)C1(CO1)C)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(CC(C)C)NC(=O)C(CCC3=CC=CC=C3)NC(=O)CN4CCOCC4 | ||
|
In vitro |
DMSO
: 100 mg/mL
(138.9 mM)
Ethanol : 50 mg/mL Water : Insoluble |
|
In vivo |
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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 |
Proteasome
(ANBL-6 cells) 5 nM
|
|---|---|
| 시험관 내(In vitro) |
Carfilzomib (PR-171)은 다발성 골수종을 포함한 다양한 세포주 및 환자 유래 신생물 세포에서 증식을 억제하고, 내재적 및 외재적 Apoptosis 신호 전달 경로와 c-Jun-N-말단 키나제(JNK) 활성화를 유도했습니다. 이는 향상된 항-MM 활성을 나타내고, 다른 약물에 대한 저항성을 극복하며, (Dex)와 시너지 효과를 나타냅니다. 이 화합물은 β5 서브유닛의 ChT-L 활성에 대해 시험관 내에서 우선적인 억제 효능을 보이며, 10 nM 용량에서 80% 이상의 억제를 나타냅니다. 저용량 Carfilzomib에 짧게 노출되면 β5 구성 20S Proteasome 및 β5i 면역 Proteasome 서브유닛에 대한 우선적인 결합 특이성을 유도합니다. 이 화합물로 펄스 처리된 ANBL-6 세포에서 카스파제 활성 측정을 통해 8시간 후 카스파제-8, 카스파제-9 및 카스파제-3 활성이 크게 증가하여 8시간 후 대조군 세포에 비해 각각 3.2배, 3.9배 및 6.9배 증가했습니다. Carfilzomib 펄스 처리된 세포에서 미토콘드리아 막 무결성은 41%(Q1 + Q2)로 감소했으며, 이는 운반체 처리된 대조군 세포의 75%와 비교됩니다. 다른 연구에서는 조혈 및 고형 악성 종양에 대한 전임상 효과도 보여주었습니다. 이는 골파괴 세포 형성 및 뼈 재흡수를 직접 억제합니다. |
| 키나아제 분석 |
카필조밉 서브유닛 프로파일링을 위한 효소결합 면역흡착 분석
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ANBL-6 세포(2 × 106개/웰)를 96웰 플레이트에 접종하고 Carfilzomib (PR-171)을 0.001~10 μM 용량으로 1시간 동안 처리합니다. 세포를 용해한 다음(20mM Tris-HCl, 0.5mM EDTA), 정제된 용해물을 중합효소 연쇄 반응(PCR) 플레이트로 옮깁니다. 무처리 ANBL-6 세포 용해물을 사용하여 6 μg 단백질/μL 농도부터 시작하여 표준 곡선을 생성합니다. 활성 부위 프로브 [biotin-(CH2)4-Leu-Leu-Leu-epoxyketone; 20 μM]를 첨가하고 실온에서 1시간 동안 배양합니다. 그런 다음 세포 용해물에 1% 도데실 황산나트륨(SDS)을 첨가하여 100°C로 가열하여 변성시킨 다음, 96웰 멀티스크린 DV 플레이트에 웰당 20 μL의 스트렙타비딘-세파로스 고성능 비드와 혼합하여 1시간 동안 배양합니다. 이 비드들을 효소결합 면역흡착 분석(ELISA) 완충액(PBS, 1% 소 혈청 알부민, 0.1% Tween-20)으로 세척하고 4°C에서 밤새 플레이트 셰이커에서 Proteasome 서브유닛에 대한 항체와 함께 배양합니다. 사용된 항체는 마우스 단클론 항-β1, 항-β2, 항-β1i 및 항-β5i, 염소 다클론 항-β2i 및 토끼 다클론 항-β5 (KLH-CWIRVSSDNVADLHDKYS 펩타이드에 대한 친화성 정제 항혈청)를 포함했습니다. 비드들을 세척하고 2시간 동안 고추냉이 과산화효소 접합 2차 염소 항-토끼, 염소 항-마우스 또는 토끼 항-염소 항체와 함께 배양합니다. 세척 후, 비드들을 슈퍼시그널 ELISA 피코화학발광 기질을 사용하여 현상합니다. 발광 검출을 수행합니다. 원시 발광은 표준 곡선과의 비교를 통해 μg/mL로 변환되고 운반체 대조군에 대한 % 억제로 표현됩니다. 곡선 맞춤은 다음 비시그모이드 용량 반응 방정식을 사용하여 생성됩니다: Y = Bottom + (Top-Bottom)/(1 + 10̂((LogEC50 − X) × HillSlope)), 여기서 X는 농도의 로그이고, Y는 % 억제이며, EC50은 50% 효과를 나타내는 이 화합물의 용량입니다.
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| 생체 내(In vivo) |
Carfilzomib (PR-171)은 생체 내 이종이식 모델에서 종양 성장을 중간 정도로 감소시킵니다. 이는 지속적 또는 일시적 치료 모방 후 다발성 골수종 세포 생존력을 효과적으로 감소시킵니다. 이 화합물은 또한 비종양성 마우스에서 해면골 부피를 증가시키고, 뼈 재흡수를 감소시키며, 뼈 형성을 향상시킵니다. |
참조 |
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| 방법 | 바이오마커 | 이미지 | PMID |
|---|---|---|---|
| Western blot | pERK / ERK / pSTAT5 / STAT5 / pPI3K / PI3K caspase-9 / caspase-8 c-PARP / PARP / caspase-3 Bcl-2 / Bcl-Xl / Mcl-1 / Bik / Bim / Bax / Bak Atg5 / Atg12 / Beclin-1 / LC3-II Noxa / Bik / Puma / Mcl-1 EGFR / HER2 / ER alpha / p-Akt(Ser473) / Akt / p-ERK / ERK / p53 BDP1 / HER2(Tyr1248) / HER2(Tyr1221/Tyr1222) / PARP1 / caspase-7 / p53 Mut HLA class I |
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24590311 |
| Growth inhibition assay | Cell viability |
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27655642 |
(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)
| NCT 번호 | 모집 | 조건 | 스폰서/협력자 | 시작일 | 단계 |
|---|---|---|---|---|---|
| NCT05552976 | Recruiting | Relapsed or Refractory Multiple Myeloma |
Bristol-Myers Squibb |
January 10 2023 | Phase 3 |
| NCT05675449 | Recruiting | Multiple Myeloma |
Pfizer |
December 14 2022 | Phase 1 |
| NCT05041933 | Unknown status | Hematological Diseases |
University Hospital Limoges |
September 15 2021 | -- |
질문 1:
How should I prepare a solution of it for an ongoing in vivo study?
답변:
It can be dissolved in 2% DMSO/30% PEG 300/dd H₂O at 10 mg/ml as a suspension, and can be dissolved in 2% DMSO/castor oil at 10 mg/ml as a clear solution.