Home Metabolism Casein Kinase 억제제 Silmitasertib (CX-4945)

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Silmitasertib (CX-4945) Casein Kinase 2 Inhibitor

제품 번호S2248

Silmitasertib (CX-4945)은 CK2 (casein kinase 2)의 강력하고 선택적인 억제제로, 세포 없는 분석에서 IC50는 1 nM이며, Flt3, Pim1 및 CDK1에 대해서는 덜 강력합니다 (세포 기반 분석에서는 비활성). 이 화합물은 Autophagy를 유도하고 apoptosis를 촉진합니다. 임상 1/2상.
Silmitasertib (CX-4945) Casein Kinase 억제제 Chemical Structure

화학 구조

분자량: 349.77

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품질 관리

배치: 순도: 99.96%
99.96

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
UM-SCC-1 Clonogenic Assay 0.5-5 μM 14 d DMSO  inhibits clonogenic survival and sphere formation 25379016
U87-MG Growth Inhibition Assay 1/5/10 μM 24/48/72 h DMSO inhibits cell growth both concentration and time dependently 25241897
MDA-MB-231 Function Assay 2/5/10 μM 4 h inhibits serine 529 phosphorylation and the expression of IL-6, IL-8 25153725
MDA-MB-231 Function Assay 2/5/10 μM 4 h decreases the constitutive phosphorylation of both p-S529-p65 and p-S129-Akt 25153725
HCT116  Apoptosis Assay 10 μM 24/48 h DMSO induces apoptosis 24686080
HCT116  Function Assay 10 μM 4 h DMSO causes ER-stress response over the p-eIF2α branch, but does not induce CHOP  24686080
ARPE-19 Function Assay 10 μM 4 h DMSO causes ER-stress response over the p-eIF2α branch, but does not induce CHOP  24686080
HCT116  Growth Inhibition Assay 10 μM 24-96 h DMSO inhibits cell growth time dependently 24686080
ARPE-19 Growth Inhibition Assay 10 μM 24-96 h DMSO inhibits cell growth time dependently 24686080
ARPE-19 Kinase Assay 5/10/20 μM 24/48 h inhibits CK2 kinase activity at a concentration of 5 μM 24686080
SUP-B15 Apoptosis Assay 6/10 μM 48 h induces apoptosis 24561792
Nalm6  Apoptosis Assay 6/10 μM 48 h induces apoptosis 24561792
SUP-B15 Function Assay 10/20 μM 24 h results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression 24561792
Nalm6  Function Assay 10/20 μM 24 h results in decreased PTEN phosphorylation at the CK2 target residue S380 and concomitant downregulation of PTEN protein expression 24561792
C2C12 Function Assay 3 μM 12/24/48 h inhibits the expression of osteoclast differentiation markers and Akt phosphorylation 24293011
MOLT-4 Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
DND-41 Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
ALL-SIL Apoptosis Assay 5 μM 24/48 h induces apoptosis 24253024
DND-41 Growth Inhibition Assay 1-10 μM 48 h IC50=9 μM 24253024
HPB-ALL Growth Inhibition Assay 1-10 μM 48 h IC50=6.1 μM 24253024
ALL-SIL Growth Inhibition Assay 1-10 μM 48 h IC50=5.7 μM 24253024
PF-382 Growth Inhibition Assay 1-10 μM 48 h IC50=4.5 μM 24253024
MOLT-4 Growth Inhibition Assay 1-10 μM 48 h IC50=5.7 μM 24253024
CEM-S Growth Inhibition Assay 1-10 μM 48 h IC50=4.6 μM 24253024
CEM-R Growth Inhibition Assay 1-10 μM 48 h IC50=4 μM 24253024
Jurkat Growth Inhibition Assay 1-10 μM 48 h IC50=4.9 μM 24253024
Rec-1 Growth Inhibition Assay 0-40 μM 48 h IC50=1.46 µM  24086494
Jeko-1 Growth Inhibition Assay 0-40 μM 48 h IC50=2.4 µM  24086494
INA-6 Growth Inhibition Assay 0-40 μM 48 h IC50=2.42 µM 24086494
U-266 Growth Inhibition Assay 0-40 μM 48 h IC50=19.8 µM  24086494
A549 Function Assay 3 μM 48 h inhibits TGF-β1-induced activation of Smad and expression of Snail and Twist 24023938
A549 Function Assay 10 μM 12/24/48 h inhibits TGF-β1-induced migration and invasion 24023938
R-LAMA84 Growth Inhibition Assay 2.5-10 μM 48 h DMSO inhibits cell growth concentration dependently 24012109
S-LAMA84 Growth Inhibition Assay 2.5-10 μM 48 h DMSO inhibits cell growth concentration dependently 24012109
R-LAMA84 Function Assay 3 μM 24 h DMSO reduces CK2 activity 24012109
S-LAMA84 Function Assay 3 μM 24 h DMSO reduces CK2 activity 24012109
A549 Function Assay 1/10 μM 48 h DMSO leads to a dose-dependent decrease in Notch reporter activity 23651443
H1299 Growth Inhibition Assay 0-30 μM 72 h DMSO IC50=1.80 μM, inhibits cell growth concentration dependently 23651443
A549 Growth Inhibition Assay 0-30 μM 72 h DMSO IC50=4.15 μM, inhibits cell growth concentration dependently 23651443
LNCap Growth Inhibition Assay 0-30 μM 4 d IC50=4.59 μM 22832316
H2170  Function Assay 10 μM 4-24 h enhances apoptosis with 22387988
A431  Function Assay 10 μM 4-24 h enhances apoptosis with 22387988
H2170  Function Assay 10 μM 30 min attenuates PI3K-Akt-mTOR signaling 22387988
A431  Function Assay 10 μM 30 min attenuates PI3K-Akt-mTOR signaling 22387988
UM-SCC-46 Clonogenic Assay 0.5-5 μM 14 d DMSO  inhibits clonogenic survival and sphere formation 25379016
H28 Growth Inhibition Assay 0.01-30 μM 72 h DMSO IC50=7.2 μM 25422081
H2052 Growth Inhibition Assay 0.01-30 μM 72 h DMSO IC50=2.0 μM 25422081
PC9/GR Function Assay 5 µM 48 h induces autophagy 25486409
PC9/ER Function Assay 5 µM 48 h induces autophagy 25486409
H1299 Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
Calu-1  Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
H358 Growth Inhibition Assay 1/5/10 μM 72 h inhibits cell growth concentration dependently 25750308
H1299 Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
Calu-1  Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
H358 Apoptosis Assay 10 μM 72 h induces apoptosis 25750308
NU-DUL Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 3 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 10 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 1 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 18 Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Oci Ly 19  Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
Raji Growth Inhibition Assay 5-25 μM 48 h inhibits cell growth concentration dependently 25788269
UM-SCC1 Growth Inhibition Assay 0.1-30 μM 1-5 d IC50=4.1 μM 25798061
UM-SCC46 Growth Inhibition Assay 0.1-30 μM 1-5 d IC50=3.4 μM 25798061
UM-SCC1 Function Assay 0.5/4/10 μM 72 h down-regulates the expression of NF-ĸB, Bcl-XL and up-regulates the expression of p53, p21, AP-1 and IL-8 concentration dependently 25798061
UM-SCC46 Function Assay 0.5/4/10 μM 72 h down-regulates the expression of NF-ĸB, Bcl-XL, p53, p21, AP-1 and up-regulates the expression IL-8 concentration dependently 25798061
HEK293 Kinase Assay 0.5 μM 15 min DMSO reduces CK2 kinase activity 25887626
Hela Kinase Assay 0.5 μM 15 min DMSO reduces CK2 kinase activity 25887626
LAMA84 Kinase Assay 0.5 μM 15 min DMSO reduces CK2 kinase activity 25887626
HEK293 Function Assay 3 μM 5 h DMSO CK2 phosphorylates eIF3j at Ser127 25887626
HDMEC Kinase Assay 1-50 μM 5 h DMSO decreases CK2 kinase activity without affecting cell viability 26189586
HDMEC Function Assay 50 μM 1/5 h DMSO decreases the nuclear signal of phosphorylated p65 in TNF-α-stimulated HDMEC  26189586
A549  Function Assay 3/10 μM 48 h suppresses the micropillar-induced expression of p-FAK 26318800
platelets Kinase Assay 1/5/10 μM 0.5 h DMSO reduces CK2 kinase activity and platelet aggregation 26381437
HDMEC Kinase Assay 0.25/0.5/1 μM 24 h DMSO reduces CK2 kinase activity, vWF expression and secretion 26381437
HDMEC Function Assay 0.25/0.5/1 μM 24 h DMSO reduces expression of VCAM-1 but not ICAM-1 26381437
HDMEC Function Assay 1 μM 24 h DMSO affects subcellular localization of NFATc1 and phospho-p65 26381437
Jurkat Function assay Inhibition of CK2 in human Jurkat cells assessed as inhibition of [gamma33P]ATP incorporation into substrate by luminescence assay, IC50 = 0.1 μM. 21174434
MIAPaCa2 Antiproliferative assay 4 days Antiproliferative activity against human MIAPaCa2 cells after 4 days by alamar blue assay, IC50 = 1.1 μM. 21174434
PC3 Antiproliferative assay 4 days Antiproliferative activity against human PC3 cells after 4 days by alamar blue assay, IC50 = 2.1 μM. 21174434
HCT116 Antiproliferative assay 4 days Antiproliferative activity against human HCT116 cells after 4 days by alamar blue assay, IC50 = 2.2 μM. 21174434
H1299 Antiproliferative assay 4 days Antiproliferative activity against human H1299 cells after 4 days by alamar blue assay, IC50 = 2.4 μM. 21174434
Jurkat Antiproliferative assay 4 days Antiproliferative activity against human Jurkat cells after 4 days by alamar blue assay, IC50 = 2.5 μM. 21174434
A549 Antiproliferative assay 4 days Antiproliferative activity against human A549 cells after 4 days by alamar blue assay, IC50 = 3 μM. 21174434
A375 Antiproliferative assay 4 days Antiproliferative activity against human A375 cells after 4 days by alamar blue assay, IC50 = 3.9 μM. 21174434
BxPC3 Antiproliferative assay 4 days Antiproliferative activity against human BxPC3 cells after 4 days by alamar blue assay, IC50 = 4.4 μM. 21174434
LNCAP Antiproliferative assay 4 days Antiproliferative activity against human LNCAP cells after 4 days by alamar blue assay, IC50 = 4.7 μM. 21174434
K562 Antiproliferative assay 4 days Antiproliferative activity against human K562 cells after 4 days by alamar blue assay, IC50 = 5.3 μM. 21174434
MDA-MB-231 Antiproliferative assay 4 days Antiproliferative activity against human MDA-MB-231 cells after 4 days by alamar blue assay, IC50 = 6.4 μM. 21174434
MCF7 Antiproliferative assay 4 days Antiproliferative activity against human MCF7 cells after 4 days by alamar blue assay, IC50 = 8.9 μM. 21174434
Hs 578T Antiproliferative assay 4 days Antiproliferative activity against human Hs 578T cells after 4 days by alamar blue assay, IC50 = 13.1 μM. 21174434
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay, IC50 = 5.2 μM. 22339433
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay, IC50 = 6.5 μM. 22339433
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, IC50 = 8.2 μM. 22339433
MV4-11 Antiproliferative assay 1 to 3 days Antiproliferative activity against human MV4-11 cells after 1 to 3 days by MTS assay, CC50 = 3 μM. 23711832
U937 Antiproliferative assay 1 to 3 days Antiproliferative activity against human U937 cells after 1 to 3 days by MTS assay, CC50 = 4.2 μM. 23711832
Jurkat Antiproliferative assay 1 to 3 days Antiproliferative activity against human Jurkat cells after 1 to 3 days by MTS assay, CC50 = 4.5 μM. 23711832
K562 Antiproliferative assay 1 to 3 days Antiproliferative activity against human K562 cells after 1 to 3 days by MTS assay, CC50 = 7 μM. 23711832
Sf9 Function assay Inhibition of CDK2/cyclin E (unknown origin) expressed in Sf9 cells using histone H1 as substrate in presence of [gamma33P]ATP, IC50 = 1.8 μM. 24681986
A549 Cytotoxicity assay 72 hrs Cytotoxicity against human A549 cells after 72 hrs by MTS assay, CC50 = 9.9 μM. 26850376
Sf21 Function assay 90 mins Inhibition of recombinant human full length N-terminal His6-tagged CK2alpha expressed in Sf21 insect cells using CK2tide as substrate treated for 20 mins measured after 90 mins in presence of MgCl2 by caliper mobility shift assay, IC50 = 0.003 μM. 29559278
Vero E6 Antiviral assay 48 h IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 3.89045 μM. 32353859
A549 Function assay 30 uM 48 hrs Inhibition of CK2-mediated MMP2 activation in human A549 cells at 30 uM after 48 hrs by gelatin-zymography 24012124
A549 Function assay 10 uM 15 to 30 mins Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM after 15 to 30 mins by Western blot method 24012124
A549 Function assay 1 to 10 uM 24 hrs Inhibition of CK2-mediated MT1-MMP expression in human A549 cells at 1 to 10 uM after 24 hrs by Western blot method 24012124
A549 Function assay 10 uM Inhibition of CK2-mediated ERK phosphorylation in human A549 cells at 10 uM by Western blot method 24012124
A549 Function assay 10 uM 24 hrs Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 24 hrs by Western blot method 24012124
A549 Function assay 10 uM 4 to 24 hrs Inhibition of CK2-mediated AKT phosphorylation in human A549 cells at 10 uM after 4 to 24 hrs by Western blot method 24012124
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
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary 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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량 349.77 화학식

C19H12ClN3O2

 보관 (수령일로부터)
CAS 번호 1009820-21-6 SDF 다운로드 원액 보관

동의어 N/A Smiles C1=CC(=CC(=C1)Cl)NC2=NC3=C(C=CC(=C3)C(=O)O)C4=C2C=CN=C4

용해도

In vitro
배치:

DMSO : 70 mg/mL (200.13 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

작용 메커니즘

특징
First clinical inhibitor of CK2.
Targets/IC50/Ki
CK2
(Cell-free assay)
1 nM
시험관 내(In vitro)

Silmitasertib (CX-4945)는 CK2에 선택적이며, 0.5 μM 농도에서 238가지 키나아제 중 7가지만 90% 이상 억제하며, 이는 CK2의 IC50보다 500배 높은 수치입니다. 세포 없는 시스템에서 이 화합물은 FLT3, PIM1, CDK1을 각각 35 nM, 46 nM, 56 nM의 IC50로 억제하지만, 10 μM 농도에서의 처리는 세포 기반 기능 분석에서 FLT3, PIM1, CDK1에 대해 비활성입니다. 이 화합물은 광범위한 항증식 활성을 보이며, 유방암 세포주는 1.71-20.01 μM의 EC50으로 가장 넓은 범위의 민감도를 나타냅니다. CX-4945의 항증식 활성은 CK2α mRNA 및 단백질 수준과 상관관계가 있지만, CK2α' 촉매 서브유닛, 조절 CK2β 서브유닛, PI3K/Akt 또는 PTEN 돌연변이 상태와는 상관관계가 없습니다. PI3K/Akt 신호 전달을 PTEN 활성화가 아닌 CK2에 의한 세린 129에서의 Akt 인산화를 직접적으로 차단하여 억제합니다. 이 화합물로 치료하면 p21 (T145) 인산화가 감소하고, 총 p21 및 p27 수준이 증가하며, 카스파제 3/7 활성이 유도됩니다. BT-474 세포에서는 G2/M 세포 주기 정지를 유도하고, BxPC-3 세포에서는 G1 정지를 유도합니다. 이 화합물은 HUVEC 증식, 이동 및 튜브 형성을 각각 5.5 μM, 2 μM, 4 μM의 IC50로 억제합니다. BT-474 및 BxPC-3 세포의 저산소 조건에서 p53 및 pVHL의 하향 조절을 방지하고 HIF-1α 전사의 활성화를 감소시킵니다. Jurkat 세포에서 0.1 μM의 IC50로 내인성 세포내 CK2 활성을 강력하게 억제합니다.

키나아제 분석
CK2 Kinase Assay
Silmitasertib (CX-4945)는 10 μL의 부피로 반응 혼합물에 첨가되며, 이 혼합물은 10 μL의 분석 희석 완충액 (ADB; 20 mM MOPS, pH 7.2, 25 mM β-글리세롤인산염, 5 mM EGTA, 1 mM 오르토바나듐산 나트륨 및 1 mM 디티오트레이톨), 10 μL의 기질 펩타이드 (RRRDDDSDDD, ADB에 1 mM 농도로 용해), 10 μL의 재조합 인간 CK2 (ααββ-홀로효소, ADB에 25 ng 용해)를 포함합니다. 반응은 10 μL의 ATP 용액 (90% 75 mM MgCl2, 75 μM ATP (최종 ATP 농도=15 μM)를 ADB에 용해; 10% [γ-33P]ATP (원액 1 mCi/100 μL; 3000 Ci/mM)를 첨가하여 시작하며, 30 °C에서 10분 동안 유지됩니다. 반응은 100 μL의 0.75% 인산으로 퀀칭된 다음 인산셀룰로오스 필터 플레이트로 옮겨져 여과됩니다. 각 웰을 0.75% 인산으로 5회 세척한 후, 플레이트는 5분 동안 진공 건조되고, 각 웰에 15 μL의 섬광액을 첨가한 후 Wallac 발광 카운터를 사용하여 잔류 방사능이 측정됩니다. 이 화합물의 IC50 값은 0.0001 μM에서 1 μM 범위의 8가지 농도에서 파생됩니다.
생체 내(In vivo)

Silmitasertib (CX-4945)를 25 mg/kg 또는 75 mg/kg 용량으로 1일 2회 경구 투여 시 BT-474 모델에서 강력한 항종양 활성을 나타내며, 각각 88% 및 97%의 TGI를 보였고, 각 그룹의 9마리 중 2마리에서 초기 종양 부피 대비 50% 이상의 종양 크기 감소를 보였습니다. BxPC-3 모델에서 이 화합물을 75 mg/kg 용량으로 1일 2회 처리 시 93%의 TGI를 보였고, 치료 기간 종료 시 3마리에서는 종양 잔존 증거가 없었습니다. PC3 이종이식 모델에서 25 mg/kg, 50 mg/kg 또는 75 mg/kg 용량으로 투여 시 각각 19%, 40%, 86%의 TGI로 종양 성장 억제를 유발했습니다.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/22387988/

적용 분야

방법 바이오마커 이미지 PMID
Western blot p-S6K1(T389) / S6K1 / p-S6(S235/236) / S6 p-AKT(S129) / p-AKT(T308) / p-AKT(S473) / AKT / p-ERK / ERK / TP53 / p-p21(Th145) / p21 / Bcl-xl p-Smad2 (Cytosol) / Smad2/3 (Cytosol) / Smad2/3 (Nucleus) / Twist / Snail
S2248-WB1
30683840
Immunofluorescence β-catenin E-cadherin / Vimentin
S2248-IF1
24023938
Growth inhibition assay Cell viability
S2248-viability1
30316146

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT05817708 Completed
COVID-19
Senhwa Biosciences Inc.
 November 7 2022 Phase 1
NCT04668209 Terminated
Coronavirus
University of Arizona|Senhwa Biosciences Inc.
 January 21 2021 Phase 2
NCT04663737 Completed
Covid19
Chris Recknor MD|Senhwa Biosciences Inc.
 December 3 2020 Phase 2
NCT03904862 Suspended
Medulloblastoma Childhood
Pediatric Brain Tumor Consortium|National Cancer Institute (NCI)|American Lebanese Syrian Associated Charities (ALSAC)
 July 25 2019 Phase 1|Phase 2
NCT02128282 Completed
Cholangiocarcinoma
Senhwa Biosciences Inc.
 June 2014 Phase 1|Phase 2

기술 지원

취급 설명서

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자주 묻는 질문

질문 1:
How to reconstitute it (S2248) for in vivo uses?

답변:
For injection, it can be dissolved in 2% DMSO+30% PEG 300+2% Tween 80+ddH2O at 5mg/ml clearly. When making the solution, please dissolve this compound in DMSO clearly first. If it dissolves not readily, please sonicate and warm the solution in water bath at about 45-50℃. Then add PEG and Tween. After they mixed well, dilute with water. For oral gavage, it can be dissolved in 1% CMC Na at 30mg/ml as a homogeneous suspension. This is a common formulation for oral gavage, and is convenience to prepare.