LY2510924

카탈로그 번호S8505 배치:S850502

기술 자료

화학식	C₆₂H₈₈N₁₄O₁₀
분자량	1189.45	CAS 번호	1088715-84-7
용해도 (25°C)*	시험관 내(In vitro)	Water	46 mg/mL (38.67 mM)


* <1 mg/ml은 약간 용해되거나 불용해됨을 의미합니다. * Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다. * 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명

LY2510924는 CXCR4에 대한 SDF-1의 결합을 0.079 nmol/L의 IC50 값으로 특이적으로 차단하고 0.38 nmol/L의 Kb 값으로 SDF-1 유도 GTP 결합을 억제하는 강력하고 선택적인 CXCR4 길항제입니다.

표적

CXCR4
(Cell-free)

0.079 nM

시험관 내(In vitro)

In human lymphoma U937 cells expressing endogenous CXCR4, LY2510924 inhibits SDF-1-induced cell migration with IC50 value of 0.26 nmol/L and inhibits SDF-1/CXCR4-mediated intracellular signaling. This compound exhibits a concentration-dependent inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells. Biochemical and cellular analyses reveal that it has no apparent agonist activity. It has no inhibitory activities against other chemokine receptors including CCR1, CCR2, CXCR2, and CXCR3 at the concentrations tested. Similarly, there is no activity observed among serotonin, dopamine, and opioid receptors.

생체 내(In Vivo)

LY2510924 has acceptable in vivo stability and a pharmacokinetic profile similar to a typical small-molecular inhibitor in preclinical species. This compound shows dose-dependent inhibition of tumor growth in human xenograft models developed with non-Hodgkin lymphoma, renal cell carcinoma, lung, and colon cancer cells that express functional CXCR4. In MDA-MB-231, a breast cancer metastatic model, it inhibits tumor metastasis by blocking migration/homing process of tumor cells to the lung and by inhibiting cell proliferation after tumor cell homing. This chemical has a dramatically improved in vivo stability with a half-life of 3 to 5 hours in preclinical species and 9.16 hours in humans at the recommended phase II dose.

프로토콜 (참조)

세포 분석:^{^[1]}	세포주 U937 cells 농도 -- 배양 시간 2.5 h 방법 U937 cells are harvested and washed once with chemotaxis assay buffer prepared with 1× RPMI medium containing 10 mmol/L HEPES, pH 7.5, and 0.3% BSA. Cells are then resuspended in assay buffer at a density of 5 × 10⁶ cells/mL. The assay is performed in a 96-well ChemoTx plate. Generally, 50 μL of cell mixture with or without this compound was plated on the upper chamber, and 30 μL of SDF-1α (10 ng/mL) prepared in 1× chemotaxis buffer was added to the lower chamber. The plate is then incubated for 2.5 hours at 37°C. Following the incubation, 5 μL of CellTiter 96 AQ is added into the lower chamber. The plate is then incubated for 60 minutes at 37°C. The migrated cells are detected by measuring the absorbance at 492 nm.
동물 연구:^{^[1]}	동물 모델 female C57/BL6 mice, male Sprague–Dawley rats, male Beagle dogs, and male Cynomolgus monkeys at fasted state 용량 3 mg/kg 투여 subcutaneous (s.c.) or intravenous (i.v.) injection

세포 분석:^{^[1]}

세포주
U937 cells
농도
--
배양 시간
2.5 h
방법
U937 cells are harvested and washed once with chemotaxis assay buffer prepared with 1× RPMI medium containing 10 mmol/L HEPES, pH 7.5, and 0.3% BSA. Cells are then resuspended in assay buffer at a density of 5 × 10⁶ cells/mL. The assay is performed in a 96-well ChemoTx plate. Generally, 50 μL of cell mixture with or without this compound was plated on the upper chamber, and 30 μL of SDF-1α (10 ng/mL) prepared in 1× chemotaxis buffer was added to the lower chamber. The plate is then incubated for 2.5 hours at 37°C. Following the incubation, 5 μL of CellTiter 96 AQ is added into the lower chamber. The plate is then incubated for 60 minutes at 37°C. The migrated cells are detected by measuring the absorbance at 492 nm.

동물 연구:^{^[1]}

동물 모델
female C57/BL6 mice, male Sprague–Dawley rats, male Beagle dogs, and male Cynomolgus monkeys at fasted state
용량
3 mg/kg
투여
subcutaneous (s.c.) or intravenous (i.v.) injection

참조

https://pubmed.ncbi.nlm.nih.gov/25504752/

Selleck's LY2510924 인용됨 3 출판물

Modeling the SDF-1/CXCR4 protein using advanced artificial intelligence and antagonist screening for Japanese anchovy [ Front Physiol, 2024, 15:1349119]	PubMed: 38370015
Modeling the SDF-1/CXCR4 protein using advanced artificial intelligence and antagonist screening for Japanese anchovy [ Frontiers in Physiology, 2024, 1349119]	PubMed: 38370015
Expansion of human megakaryocyte-biased hematopoietic stem cells by biomimetic Microniche [ Nat Commun, 2023, 14(1):2207]	PubMed: 37072407

반품 정책
Selleck Chemical의 무조건 반품 정책은 고객에게 원활한 온라인 쇼핑 경험을 보장합니다. 구매에 어떤 식으로든 불만족하시면, 수령일로부터 7일 이내에 모든 품목을 반품하실 수 있습니다. 제품 품질 문제(프로토콜 관련 문제 또는 제품 관련 문제)가 발생하는 경우, 원래 구매일로부터 365일 이내에 모든 품목을 반품하실 수 있습니다. 제품 반품 시 아래 지침을 따르십시오.

배송 및 보관
Selleck 제품은 실온에서 운송됩니다. 실온에서 제품을 받으셨더라도 안심하십시오. Selleck 품질 검사 부서에서 한 달간의 상온 보관이 분말 제품의 생물학적 활성에 영향을 미치지 않음을 확인하는 실험을 수행했습니다. 수령 후, 데이터시트에 설명된 요구 사항에 따라 제품을 보관하십시오. 대부분의 Selleck 제품은 권장 조건에서 안정적입니다.

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