Home Neuronal Signaling Adenosine Deaminase inhibitor Cladribine

연구용

Cladribine Adenosine Deaminase inhibitor

제품 번호: S1199

Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.
Cladribine Adenosine Deaminase inhibitor Chemical Structure

화학 구조

분자량: 285.69

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품질 관리 (Quality Control)

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
CCRF-CEM cell lines Cytotoxicity assay Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.003 μM 1732556
HEp-2 cell lines Cytotoxicity assay Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.03 μM 1732556
L1210 cell lines Cytotoxicity assay Compound was tested for cytotoxicity against L1210 cell lines, IC50=0.07 Μm 1732556
CCRF-CEM cells Cytotoxicity assay 72 h Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay, IC50=0.0005 μM 21840722
human Raji cells Cytotoxicity assay 72 h Cytotoxicity against human Raji cells after 72 hrs by MTT assay, IC50=0.009 μM 21840722
human HuH7 cells Cytotoxicity assay 72 h Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay, IC50=1.8 μM 25462277
human T47D cells Cytotoxicity assay 72 h Cytotoxicity against human T47D cells after 72 hrs by SRB assay, IC50=0.7 μM 25462277
human HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.3 μM 25462277
human K562 cells Proliferation assay 48 h Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=10 μM 25960323
human SKHEP1 cells Proliferation assay 48 h Antiproliferative activity against human SKHEP1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=4 μM 25960323
human MOLT3 cells Proliferation assay 48 h Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2.3 μM 25960323
human KG1 cells Proliferation assay 48 h Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.2 μM 25960323
human RPMI8226 cells Proliferation assay 48 h Antiproliferative activity against human RPMI8226 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM 25960323
human MCF7 cells Proliferation assay 48 h Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=45 μM 25960323
human SK-UT-1B cells Proliferation assay 48 h Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=1 μM 25960323
L1210 cell lines Function assay In vitro inhibitory effect was tested for cytostatic activity on the growth of murine leukemic L1210 cell lines, ID50=0.03 μM 2995666
P388 leukemic cell lines Function assay In vitro inhibitory effect was tested for cytostatic activity on the growth of lymphoid neoplasm P388 leukemic cell lines, ID50=0.03 μM 2995666
BV173 Cytotoxicity assay 3 days Cytotoxicity against human BV173 cells after 3 days by MTT assay, IC50=0.0008μM 21711054
BT549 Cytotoxicity assay 3 days Cytotoxicity against human BT549 cells after 3 days by MTT assay, IC50=0.123μM 21711054
CT26 Cytotoxicity assay 3 days Cytotoxicity against mouse CT26 cells after 3 days by MTT assay, IC50=0.131μM 21711054
MES-SA Cytotoxicity assay 3 days Cytotoxicity against human MES-SA cells after 3 days by MTT assay, IC50=0.165μM 21711054
K562 Cytotoxicity assay 3 days Cytotoxicity against human paclitaxel resistant K562 cells after 3 days by MTT assay, IC50=0.17μM 21711054
P388D1 Cytotoxicity assay 3 days Cytotoxicity against mouse P388D1 cells after 3 days by MTT assay, IC50=0.285μM 21711054
CEM-DNR-bulk Cytotoxicity assay 3 days Cytotoxicity against human CEM-DNR-bulk cells after 3 days by MTT assay, IC50=0.352μM 21711054
L1210 Cytotoxicity assay 3 days Cytotoxicity against mouse L1210 cells after 3 days by MTT assay, IC50=0.393μM 21711054
EL4 Cytotoxicity assay 3 days Cytotoxicity against mouse EL4 cells after 3 days by MTT assay, IC50=0.848μM 21711054
MCF7 Cytotoxicity assay 3 days Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=2.35μM 21711054
K562 Cytotoxicity assay 3 days Cytotoxicity against human K562 cells after 3 days by MTT assay, IC50=7.69μM 21711054
PC3 Cytotoxicity assay 3 days Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=8.28μM 21711054
C6 Cytotoxicity assay 3 days Cytotoxicity against rat C6 cells after 3 days by MTT assay, IC50=9.07μM 21711054
HPAC Cytotoxicity assay 3 days Cytotoxicity against human HPAC cells after 3 days by MTT assay, IC50=9.32μM 21711054
HCT116 Cytotoxicity assay 3 days Cytotoxicity against human HCT116 cells after 3 days by MTT assay, IC50=9.43μM 21711054
HT-29 Cytotoxicity assay 3 days Cytotoxicity against human HT-29 cells after 3 days by MTT assay, IC50=9.44μM 21711054
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=0.3μM 28219046
HuH7 Cytotoxicity assay 72 hrs Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=1.8μM 28219046
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=2μM 28219046
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 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
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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: Confirmatory screen for MG 63 (6-TG R) cells 29435139
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 285.69 화학식

C10H12ClN5O3

 보관 (수령일로부터)
CAS 번호 4291-63-8 SDF 다운로드 원액 보관

동의어 2-CdA,2-Chloro-2′-deoxyadenosine,CldAdo,Jk 6251,NSC 105014,RWJ 26251 Smiles C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)O

용해도 (Solubility)

In vitro
배치:

DMSO : 57 mg/mL (199.51 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 (Mechanism of Action)

특징
Cladribine is primarily active in lymphoid tissues.
Targets/IC50/Ki
Adenosine deaminase (MM1.S cells)
0.18 μM
Adenosine deaminase (RPMI8226 cells)
0.75 μM
Adenosine deaminase (U266 cells)
2.43 μM
시험관 내(In vitro)
Cladribine은 만성 B세포 림프구 증식성 질환인 모세포 백혈병(HCL)에서 놀라운 활성을 나타내며, 장기간의 완전 관해를 유도합니다. 이 화합물은 림프구 내에서 DNA 가닥 절단 축적을 유도하고, 결과적으로 종양 억제 인자인 p53을 활성화합니다. 또한 MM 세포에서 STAT3 활성을 조절할 수 있습니다. 이 화학물질은 U266, RPMI8226 및 MM1.S 세포의 증식/생존을 농도 의존적으로 억제합니다. U266이 가장 덜 민감한 세포주인 반면, MM1.S는 Cladribine에 가장 민감합니다. 이 화합물로 처리하면 세포 주기 중 G1 단계의 세포 비율이 점진적으로 증가하고 S 단계의 세포 비율이 감소합니다. 24시간 처리 시 U266 세포에서 G2-M 단계를 증가시키는 것으로 보입니다. 이 제제에 의해 유도된 세포 사멸의 농도 의존적 증가는 RPMI8226 및 MM1.S 세포 모두에서 관찰됩니다. 0.2 μM 농도로 처리하면 MM1.S 세포에서 caspase-3, -8, -9의 활성화와 PARP 절단이 시간 의존적으로 극적으로 유도됩니다. 이 화합물은 phospho-STAT3(P-STAT3) 수준을 농도 의존적으로 유의하게 감소시키지만, 총 STAT3 단백질 수준에는 영향을 미치지 않습니다. 이 화합물은 HSB2 세포에서 농도 의존적인 세포 사멸 유도 잠재력을 가지고 있습니다. 이 화학물질은 일차 비만 세포(MC) 및 MC 세포주인 HMC-1의 성장을 농도 의존적으로 억제하며, KIT D816V를 보유한 HMC-1.2 세포에서 KIT D816V가 없는 HMC-1.1 세포보다 낮은 IC50 값이 기록되었습니다. 이는 CD14+ 단핵구와 CD4+ 및 CD8+ T 림프구의 이동 능력을 감소시킵니다.
생체 내(In vivo)
Cladribine (0.7-3.5 mM) 및/또는 diltiazem (2.4 mM)을 성체 제브라피쉬에 복강 내 주사하고 적혈구(RBC) 용해물을 HPLC로 분석하여 심혈관 건강의 잠재적 바이오마커인 퓨린 뉴클레오타이드(예: ATP) 수치를 측정한다. Diltiazem은 RBC ATP 농도를 증가시켰으며, 이는 이 화합물의 동시 주입에 의해 억제된다. 이 화학 물질의 혈장 농도는 ia 및 s.c. 투여 후 2상 감소를 거쳐 빠르게 감소한다. 1 mg/kg ia 및 2 mg/kg s.c. 단일 주사 후 이 화합물의 AUC 및 t 1/2 beta는 각각 0.66 대 1.2 μg × h/mL 및 3.5 대 4.5시간이다.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/19175384/
  • [5] https://pubmed.ncbi.nlm.nih.gov/20001707/
  • [6] https://pubmed.ncbi.nlm.nih.gov/19326772/
  • [7] https://pubmed.ncbi.nlm.nih.gov/12373351/

임상시험 정보 (Clinical Trial Information)

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

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT05797740 Recruiting
Multiple Sclerosis
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 August 3 2023 --
NCT04997148 Completed
Relapsing-Remitting Multiple Sclerosis
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany|Merck Serono Limited an affiliate of Merck KGaA Darmstadt Germany
 August 11 2021 --