Name: Avapritinib (BLU-285)
Brand: Selleck Chemicals
SKU: S8553
Rating: 5 (14 reviews)

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품질 관리

배치: 순도: 99.99%

99.99

관련 타겟	EGFR VEGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
기타 PDGFR 억제제	CP-673451 Orantinib (SU6668) Tyrphostin AG 1296 Trapidil PP121 AZD2932 Sennoside B Tyrphostin AG1433 Seralutinib (GB002) N-(p-Coumaroyl) Serotonin

세포 배양, 처리 및 작업 농도

세포주	분석 유형	배양 시간	활성 설명	PMID
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.008 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.01 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.017 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.019 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.022 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.028 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.029 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.034 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.034 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.042 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.069 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.078 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.117 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.167 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.292 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.427 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.751 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.86 μM.	30204441
BA/F3 cells	Cytotoxicity assay	72 h	Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 4.075 μM.	30204441
BA/F3 cells	Growth inhibiton assay	72 h	Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 4.952 μM.	30204441
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	498.56	화학식	C₂₆H₂₇FN₁₀	보관 (수령일로부터)	3년-20°C분말
CAS 번호	1703793-34-3	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	BLU-285			Smiles	CC(C1=CC=C(C=C1)F)(C2=CN=C(N=C2)N3CCN(CC3)C4=NC=NN5C4=CC(=C5)C6=CN(N=C6)C)N

용해도

In vitro
배치:

DMSO : 100 mg/mL (200.57 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 1.5 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (200.57 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (200.57 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 2 mg/mL

Water : Insoluble

DMSO : 66 mg/mL (132.38 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 3 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (200.57 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 2 mg/mL

Water : 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.
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	2%DMSO 1 40%PEG300 2 2%Tween80 3 56%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	4.000mg/ml (8.02mM)	Taking the 1 mL working solution as an example, add 20 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 560 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.

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

Targets/IC₅₀/Ki	PDGFRα (D842V) 0.5 nM c-Kit (D816V) 0.5 nM
시험관 내(In vitro)	Avapritinib (BLU-285)은 KIT Exon 17 및 PDGFR D842 활성화 루프 돌연변이를 표적으로 하는 선택적 경구 억제제입니다. KIT 돌연변이 자가인산화 억제를 측정하는 세포 분석은 치료 불응성 GIST에서 발견되는 KIT D816 돌연변이 D816V (HMC1.2 세포, IC50 = 3 nM) 및 D816Y (P815 세포, IC50 = 22 nM)뿐만 아니라 N822K (Kasumi 세포, IC50 = 40 nM)와 같은 다른 KIT Exon 17 돌연변이에 대한 활성을 확인합니다.
생체 내(In vivo)	생체 내에서 Avapritinib (BLU-285)은 D816Y 유발 이종이식 모델에서 용량 의존적인 종양 성장 억제를 달성하는 잘 용인되고 경구 생체 이용 가능한 약물입니다. 이 화합물과 PK-PD-효능 관계가 확립되어 종양 퇴행이 90% 이상의 표적 억제에서 비롯되며 1일 1회 30 mg/kg 투여 시 관찰됨을 보여줍니다. PDGFR D842V 및 KIT Exon 17 돌연변이에 대한 강력한 활성을 통해 이전에 해결되지 않았던 질병의 유전체학적 동인을 표적으로 하며, 환자의 90% 이상이 KIT D816V 돌연변이를 보유하는 PDGFR D842V 유발 GIST(위장관 기질 종양) 또는 SM(전신 비만세포증) 치료에 대한 가능성을 제공합니다. 단일 제제 활성 외에도 고도로 선택적인 BLU-285는 GIST에서 KIT의 전체적인 원발성 및 내성 돌연변이를 커버하기 위해 다른 제제와의 병용 기회를 제공합니다.
참조	[1] http://cancerres.aacrjournals.org/content/75/15_Supplement/791 [2] https://aacrjournals.org/cancerres/article/75/15_Supplement/791/605110/Abstract-791-BLU-285-the-first-selective-inhibitor

적용 분야

방법	바이오마커	이미지	PMID
Western blot	PDGFRA / c-KIT / Wee1 / Cdc2 / PARP / γH2AX / CyclinD1 / β-actin		33320833

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT04908176	Completed	Gastrointestinal Stromal Tumors\|GIST\|Non-resectable Advanced Solid Tumors\|Recurrent or Unresectable Central Nervous System (CNS) Tumors	Blueprint Medicines Corporation	August 24 2022	Phase 1
NCT04695431	Completed	Advanced Systemic Mastocytosis\|Aggressive Systemic Mastocytosis\|Systemic Mastocytosis With an Associated Hematological Neoplasm\|Mast Cell Leukemia	Blueprint Medicines Corporation\|Analysis Group Inc.	December 2 2020	--
NCT03731260	Active not recruiting	Indolent Systemic Mastocytosis	Blueprint Medicines Corporation	April 16 2019	Phase 2
NCT03580655	Active not recruiting	Advanced Systemic Mastocytosis\|Aggressive Systemic Mastocytosis\|Systemic Mastocytosis With an Associated Hematologic Neoplasm\|Mast Cell Leukemia	Blueprint Medicines Corporation	November 21 2018	Phase 2
NCT03465722	Completed	GIST	Blueprint Medicines Corporation	March 26 2018	Phase 3

기술 지원

취급 설명서

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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):

Avapritinib (BLU-285) PDGFR 억제제

화학 구조

분자량: 498.56

품질 관리

세포 배양, 처리 및 작업 농도

화학 정보, 보관 및 안정성

용해도

몰농도 계산기

생체 내 제형 계산기 (투명한 용액)

작용 메커니즘

적용 분야

임상시험 정보

기술 지원