CTX1
Catalog No.: GC32911Purity:>98.00%
CTX1은 HdmX 매개 p53 억제를 극복하는 p53 활성제입니다. CTX1은 마우스 급성 골수성 백혈병(AML) 모델 시스템에서 강력한 항암 활성을 나타냅니다.
제품은 연구용으로만 사용됩니다. 인체에 사용할 수 없으며 환자에게 판매하지 않습니다.
Cas No.: 501935-96-2
10mM (in 1mL DMSO)In Stock
$232.00
1
1mgIn Stock
$117.00
1
5mgIn Stock
$243.00
1
10mgIn Stock
$428.00
1
25mgIn Stock
$891.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $232.00 | In Stock | 1 | |
| 1mg | $117.00 | In Stock | 1 | |
| 5mg | $243.00 | In Stock | 1 | |
| 10mg | $428.00 | In Stock | 1 | |
| 25mg | $891.00 | In Stock | 1 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
인용 문헌 (Citations)
1 publications이 제품을 사용한 연구자들의 논문제품 설명 (Description)
CTX1 is a novel small molecule p53 activator.
CTX1 induces significant p53-dependent cell death preferentially in HdmX-expressing cells as compare to cells in which p53 is inactivated by Hdm2 overexpression or p53 is knocked down using p53 targeting shRNA. CTX1 can induce p53 protein levels in the p53 mutant cell line, HT29. It is also found that CTX1 exhibits potent activity (LD50 ~1 μM) as a single agent on primary AML patient samples in a similar fashion to AML cell lines. After 16 hr of treatment with CTX1 in HCT116 p53-wild-type cells there is a decrease in S phase from 23% to 3% while HCT116 p53-null cells exhibit a reduction in S phase from 34% to 28%. The combination of low doses of CTX1 and nutlin-3 leads to a significant enhancement of apoptosis in p53-wildtype, but not p53-null cells[1].
CTX1 even as a single agent significantly enhances the survival of mice in this model system. Mice treated with CTX1 alone or in combination with nutlin-3 has a significantly increased survival time (p<0.0001)[1].
[1]. Karan G, et al. Identification of a Small Molecule That Overcomes HdmX-Mediated Suppression of p53. Mol Cancer Ther. 2016 Apr;15(4):574-582.
실험 프로토콜 (Protocol)
Kinase experiment: | Exponentially growing OCI cells cultures are treated with 3 μM CTX1, 8 μM Nutlin and or 15 μM RO-5963 for 4.5 hrs. Whole-cell extracts are generated using modified RIPA lysis buffer 25 mM Tris (pH 8.0), 100 mM NaCl, 0.5 mM EDTA, 0.50% NP-40 and complete protease mixture tablet. Protein extracts (~750 μg) are precleared and immune precipitation is performed using a kit according to the manufacturer's protocol. For the immunoprecipitation, mouse monoclonal anti-p53 and rabbit polyclonal anti-HDMX are used. Immune complexes are then collected, proteins are eluted and subjected to Western blotting with the indicated antibodies[1]. |
Animal experiment: | 6 week old female NOD/SCID/IL2Rγ−/− mice are injected into the tail vein with 5×106 cells primary human AML cells (n=5 per group). Drug treatment is started 2 days after tumor cell injection. Nutlin-3 is given by oral gavage (200 mg/kg) and CTX1 is injected i.p. (30 mg/kg) five days a week for 3 weeks. Flow cytometry is performed on bone marrow cells isolated from the mouse femur using a human specific CD45PE antibody using a cytometer to confirm AML infiltration into the bone marrow[1]. |
References: [1]. Karan G, et al. Identification of a Small Molecule That Overcomes HdmX-Mediated Suppression of p53. Mol Cancer Ther. 2016 Apr;15(4):574-582. | |
제품 문서 (Product Documents)
Purity:>98.00%Appearance:A solid
화학적 특성 (Chemical Properties)
CAS 번호
501935-96-2
SMILES
N#CC1=C(C=CC(N)=C2)C2=NC3=CC(N)=CC=C31
분자식
C14H10N4
분자량
234.26
용해도
Soluble in DMSO
보관
Store at -20°C
일반 주의사항
제품의 용해도 데이터에 따라 적절한 용매를 선택하십시오. 조제 후에는 반복적인 동결·해동을 피할 수 있도록 저장 용액을 소분하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
저장 용액은 -80°C 보관 시 6개월 이내, -20°C 보관 시 1개월 이내에 사용하십시오.
용해도를 높이려면 튜브를 37°C로 데운 뒤 적절한 시간 동안 초음파 처리하십시오.
배송 조건
평가용 샘플은 아이스팩과 함께 배송됩니다. 그 외 용량은 실온 배송되며, 요청 시 아이스팩과 함께 배송할 수 있습니다.
계산 도구 (Calculators)몰 농도 / 희석 / 분자량 / 단위 변환 / 생체 내 제형 / 용해도
g/mol
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