Name: BMS-536924
Brand: Selleck Chemicals
SKU: S1012
Rating: 5 (26 reviews)

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품질 관리 (Quality Control)

배치: 순도: 99.98%

99.98

관련 타겟	EGFR VEGFR FGFR PDGFR c-Met Src MEK CSF-1R HER2 FLT3
기타 IGF-1R 억제제	Linsitinib (OSI-906) NVP-AEW541 BMS-754807 Picropodophyllin (AXL1717) AG-1024 GSK1904529A NVP-ADW742 NT157 PQ 401 MSDC-0160

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

분자량	479.96	화학식	C₂₅H₂₆ClN₅O₃	보관 (수령일로부터)	3년-20°C분말
CAS 번호	468740-43-4	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	CS-0117			Smiles	CC1=CC(=CC2=C1N=C(N2)C3=C(C=CNC3=O)NCC(C4=CC(=CC=C4)Cl)O)N5CCOCC5

용해도 (Solubility)

In vitro
배치:

DMSO : 96 mg/mL (200.01 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 96 mg/mL (200.01 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 96 mg/mL (200.01 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 96 mg/mL (200.01 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	30%PEG400 1 0.5%Tween80 2 5%propylene glycol Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	30.000mg/ml (62.51mM)	Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL 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.

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	Insulin Receptor 73 nM IGF-1R 100 nM FAK 150 nM MEK 182 nM LCK 341 nM VEGFR2 1.4 μM EGF 1.6 μM Met 4.87 μM
시험관 내(In vitro)	BMS-536924 also inhibits FAK and Lck with IC50 of 150 nM and 341 nM, respectively. This compound inhibits cellular proliferation and disrupts Akt and MAPK phosphorylation. It inhibits IGF-I-stimulated IGF-1R signaling in MCF10A cells and blocks constitutive IGF-1R activity in CD8-IGF-1R-MCF10A. Preincubation of MCF10A cells with 1 μM of this chemical completely blocks the ability of IGF-I to stimulate IGF-1R phosphorylation. IGF-I stimulation results in increased phosphorylation of ERK1/2, GSK3β, and Akt. This compound inhibits this ligand-induced phosphorylation. Treatment of the CD8-IGF-1R-MCF10A cells with this inhibitor results in a dose-dependent inhibition of phosphorylation with partial inhibition at 0.01 μM and 0.1 μM, but complete receptor inhibition at a concentration of 1 μM. Maximal inhibition of phosphorylated IGF-1R is observed as early as 10 minutes following incubation. It retains its ability to inhibit IGF-1R phosphorylation for up to 48 hours. Addition of this agent time-dependently inhibits Akt phosphorylation starting at 1 hour. By 48 hours, Akt activation is completely blocked. Treatment with this compound shows antiproliferation activity in a panel of cancer cell lines including TC32, HT1080/S, SK-LMS-1, H513 and CTR cells. pIGF-1R/pIR is activated upon IGF-I/insulin stimulation and the activation is inhibited by this chemical at similar potencies in Rh41 and Rh36 cell lines. The expression of programmed cell death 4 (PDCD4), cleavage of poly(ADP-ribose) polymerase (PARP) and caspase-3 are up-regulated in Rh41 cells treated with this inhibitor.
키나아제 분석	IGF-1R 경로 활성
키나아제 분석	1 × 10⁶개의 pBabe-MCF10A 세포를 60mm 디쉬에 분주합니다. 24시간 후, 배지를 혈청이 없는 배지로 교체하고 37 °C에서 밤새 24시간 동안 배양합니다. 그 후 세포를 혈청이 없는 배지에서 1 uM BMS-536924를 처리하거나 처리하지 않은 상태로 1시간 동안 전배양한 다음, IGF-I(50 ng/mL)로 10분 동안 자극합니다. 세포 단층을 PBS로 두 번 세척하고 면역블롯 분석을 위해 수확합니다.
생체 내(In vivo)	Oral administration of BMS-536924 at 100-300 mpk strongly inhibits IGR-1R Sal tumor model. Efficacy is also observed in the nonengineered Colo205 human colon carcinoma mode. Oral administration of this compound on a once a day schedule (100-300 mpk) or a twice a day schedule (50, 100 mpk) demonstrates antitumor activity in this tumor model. Oral glucose tolerance test (OGTT) shows 100 mpk (b.i.d.) causes a significant elevation in glucose levels after glucose challenge. The pharmacokinetic parameters of this chemical, administered orally in poly(ethylene glycol) 400 and water (80:20 v/v), are determined in mouse, rat, dog, and monkey. Good bioavailability is evident in all species. Significant nonlinear pharmacokinetics is observed in rodents at increasing p.o. dose. This compound reduces the tumor xenografts volume of CD8-IGF-1R-MCF10A cells after two weeks' treatment (100mg/kg) to 76%. Oral administration of 70 mg/kg this chemical significantly inhibits tumor growth (TGBC-1TKB cells) inoculated in nude mice. It up regulates apoptosis in xenografts tumors. The treatment doesn't have adverse effects on the body weight of mice or the glucose levels at the time of death, suggesting tolerable toxicity.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/16134929/ [2] https://pubmed.ncbi.nlm.nih.gov/19118050/ [3] https://pubmed.ncbi.nlm.nih.gov/19117999/ [4] https://pubmed.ncbi.nlm.nih.gov/22044563/ [5] https://pubmed.ncbi.nlm.nih.gov/18765832/ [6] https://pubmed.ncbi.nlm.nih.gov/19117999/

자주 묻는 질문 (Frequently Asked Questions)

질문 1:
What are the differences between it and S1034?

답변:
The most remarkable difference between these two IGF-IR inhibitors is that S1012 is an ATP-competitive inhibitor. You will get more information about the differences between IR inhibitors in this reference: http://www.sciencedirect.com/science/article/pii/S1359644605035129.

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):

BMS-536924 IGF-1R 억제제

분자량: 479.96

품질 관리 (Quality Control)

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

용해도 (Solubility)

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘 (Mechanism of Action)

자주 묻는 질문 (Frequently Asked Questions)