Name: Prexasertib (LY2606368) Dihydrochloride
Brand: Selleck Chemicals
SKU: S7178
Rating: 5 (47 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.88%

99.88

함께 자주 사용되는 제품 Prexasertib (LY2606368) Dihydrochloride

Samotolisib (LY3023414)

The combination of it and LY3023414 results in tumor regression in OV-90 and Cov504 tumors and significantly enhanced efficacy when compared to singe agent.

관련 타겟	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
기타 Chk 억제제	CCT245737 (SRA737) AZD7762 Rabusertib (LY2603618) MK-8776 (SCH 900776) CHIR-124 PF-477736 Prexasertib (LY2606368) BML-277 (Chk2 Inhibitor II) GDC-0575 SAR-020106

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

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
HeLa cells	Function assay	33 or 100 nmol/L	7 hours	by 7 hours, a subpopulation of cells stained strongly for DSB by both TUNEL and pH2AX	26141948
U-2 OS cells	Function assay	4 nmol/L	24 h	a large shift in cell-cycle populations from G1 and G2–M to S-phase with an accompanied induction of H2AX phosphorylation.	26141948
CCRF-CEM parental cells	Function assay	10 nM	4 h	induced SLFN11 binding to chromatin and increased the chromatin binding of CDC45	29395061
SLFN11-del cells	Function assay	10 nM	4 h	induced SLFN11 binding to chromatin and increased the chromatin binding of CDC45	29395061
K562-WT	Function assay	100 nM	2 h	SLFN11, CDC45 and PCNA were enriched on nascent DNA	29395061
K562-E669Q	Function assay	100 nM	2 h	SLFN11, CDC45 and PCNA were enriched on nascent DNA	29395061
CCRF-CEM parental cells	Function assay	100 nM	2 h	SLFN11, CDC45 and PCNA were enriched on nascent DNA	29395061
HCT-116 cells	Function assay		10 days	inhibited both FANCD2 ubiquitination and increased Rad51 levels, significantly increased sensitivity of HCT-116 cells to F10	30439567
U937 cells	Function assay	3 nM		enhanced the cytotoxicity of CPX-351 at low nanomolar concentrations	30837643
KB-3-1	Function assay			P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	31515284
KB-8-5-11	Function assay			P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen, Potency = 1.2995 μM.	31515284
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량	438.31	화학식	C₁₈H₁₉N₇O₂.2HCl	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1234015-54-3	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	N/A			Smiles	COC1=C(C(=CC=C1)OCCCN)C2=CC(=NN2)NC3=NC=C(N=C3)C#N.Cl.Cl

용해도 (Solubility)

In vitro
배치:

DMSO : 17 mg/mL (38.78 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 14 mg/mL (31.94 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 9 mg/mL (20.53 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 30 mg/mL (68.44 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 2 mg/mL (4.56 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:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.500mg/ml (1.14mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	0.800mg/ml (1.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

생체 내 제형 계산기 (투명한 용액)

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

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

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)

Targets/IC₅₀/Ki	Chk1 (Cell-free assay) 0.9 nM(Ki) Chk2 (Cell-free assay) 8 nM RSK (Cell-free assay) 9 nM
시험관 내(In vitro)	In nonclinical studies, Prexasertib HCl (LY2606368) induced DNA damage as measured by replication catastrophe and increases in pH2A.X, a marker of double-stranded DNA breaks. Treatment of cells with this compound results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population. In a functional assay, it potently abrogated the G2–M checkpoint activated by doxorubicin in p53-deficient HeLa cells with an EC50 of 9 nmol/L. It was broadly antiproliferative with IC50 values typically <50 nmol/L in the most sensitive cell lines with a minority of cell lines showing considerable resistance with IC50's >1,000 nmol/L. This compound requires CDC25A and CDK2 to cause DNA damage.
생체 내(In vivo)	Prexasertib HCl (LY2606368) inhibited tumor growth in cancer xenografts as monotherapy and in combination with other agents. In an orthotopic SKOV3 ovarian cancer model, it was shown to inhibit the growth of primary tumors and significantly reduce the incidence of metastases and ascites accumulation. This compound also demonstrated efficacy in an SW1990 orthotopic pancreatic cancer model resulting in a 92% inhibition of primary tumor growth and the elimination of metastases to the lymphnode, spleen, and intestine.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/27044938/ [2] https://pubmed.ncbi.nlm.nih.gov/26141948/ [3] https://pubmed.ncbi.nlm.nih.gov/24140082/

적용 분야 (Applications)

방법	바이오마커	PMID
Western blot	CHK1 / p-CHK1(Ser345) / γH2AX / Cleaved caspase3 pS6 (S235/236) / pS6 (S240/244)	28401005
Immunofluorescence	SLFN11 / CDC45 / EdU	29395061
Growth inhibition assay	Cell viability IC50	28401005

임상시험 정보 (Clinical Trial Information)

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT04095221	Active not recruiting	Desmoplastic Small Round Cell Tumor\|Rhabdomyosarcoma	Memorial Sloan Kettering Cancer Center	September 17 2019	Phase 1\|Phase 2
NCT03495323	Completed	Cancer	Dana-Farber Cancer Institute\|Eli Lilly and Company	May 16 2018	Phase 1
NCT03414047	Completed	Ovarian Cancer	Eli Lilly and Company	April 10 2018	Phase 2
NCT03057145	Completed	Solid Tumor	Geoffrey Shapiro MD PhD\|Eli Lilly and Company\|AstraZeneca\|Dana-Farber Cancer Institute	March 10 2017	Phase 1

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
Would you please suggest a suitable vehicle to dissolve it for in vivo use?

답변:
It can be dissolved in a vehicle: 5% DMSO+40%PEG 300+5%Tween80+ddH2O for in vivo use in mice (i.p.). This stock concentration reaches 10mg/ml, and can be prepared for work solution as 0.5mg/ml, stable for no longer than 30min.

질문 2:
What is the solubility of it in 20% Captisol?

답변:
It is a suspension in 20% Captisol, which is fine for oral gavage. You can dissolve this compound in this vehicle to the concentration you need as long as the suspension is homogeneous.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Prexasertib (LY2606368) Dihydrochloride CHK1 Inhibitor

화학 구조

분자량: 438.31

품질 관리 (Quality Control)

함께 자주 사용되는 제품 Prexasertib (LY2606368) Dihydrochloride

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

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

자주 묻는 질문 (Frequently Asked Questions)

Prexasertib (LY2606368) Dihydrochloride CHK1 Inhibitor

화학 구조

분자량: 438.31

품질 관리 (Quality Control)

함께 자주 사용되는 제품 Prexasertib (LY2606368) Dihydrochloride

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

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

적용 분야 (Applications)

임상시험 정보 (Clinical Trial Information)

자주 묻는 질문 (Frequently Asked Questions)

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