Rebastinib|1020172-07-9|(DCC-2036)-陌孚医药/Medlife

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Rebastinib (Synonyms: DCC-2036)

目录号: PL11440 纯度: ≥99%

Rebastinib (DCC-2036) 是一种口服有效的，非 ATP 竞争性的 Bcr-Abl 抑制剂，作用于 Abl1^WT 和 Abl1^T315I，IC50 分别为 0.8 nM 和 4 nM，也抑制 SRC，KDR，FLT3 和 Tie-2，低活性作用于c-Kit。

CAS No. :1020172-07-9

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中文名称	Rebastinib
中文别名	DCC-2036 (Rebastinib) 抑制剂;N-[3-叔丁基-1-(喹啉-6-基)-1H-吡唑-5-基]-N'-[2-氟-4-[(2-(甲基氨基甲酰基)吡啶-4-基)氧]苯基]脲
英文名称	Rebastinib
英文别名	DCC-2036;2H-Cyclopenta[b]furan-2-one, 5-(benzoyloxy)-4-(4,4-difluoro-3-oxo-1-octenyl)hexahydro-, [3aR-[3aa,4a(E),5b,6aa]]-;DCC-2036 (Rebastinib);2H-Cyclopenta[b]furan-2-one, 5-(benzoyloxy)-4-(4,4-difluoro-3-oxo-1-octenyl)hexahydro-, [3aR-[...;4-(4-(3-(3-(tert-Butyl)-1-(quinolin-6-yl)-1H-pyrazol-5-yl)ureido)-3-fluorophenoxy)-N-methylpicolinamide;4-[4-[(5-tert-butyl-2-quinolin-6-ylpyrazol-3-yl)carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;Rebastinib;1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea;4-[4-({[3-Tert-Butyl-1-(Quinolin-6-Yl)-1h-Pyrazol-5-Yl]carbamoyl}amino)-3-Fluorophenoxy]-N-Methylpyridine-2-Carboxamide;DCC2036;Rebastinib [USAN];N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(methylcarbamoyl)pyridin-4-yl)oxy]phenyl]urea;Rebastinib Tosylate;Rebastinib(DCC-2036);4-(4-(3-(3-(tert-Butyl)-1-(quinolin-6-yl)-1H-pyrazol-5-yl)ureido)-3-fluorophenoxy)-N-methylpic;N-[3-tert-Butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl]-N'-[2-fluoro-4-[(2-(MethylcarbaMoyl)pyridin-4-yl);DCC 2036;75017Q6I97;4-[4-[(5-Tert-butyl-2-qu
Cas No.	1020172-07-9
分子式	C₃₀H₂₈FN₇O₃
分子量	553.59
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Rebastinib (DCC-2036) 是一种口服有效的，非 ATP 竞争性的 Bcr-Abl 抑制剂，作用于 Abl1^WT 和 Abl1^T315I，IC₅₀ 分别为 0.8 nM 和 4 nM，也抑制 SRC，KDR，FLT3 和 Tie-2，低活性作用于c-Kit。

生物活性

Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor for Abl1 and Abl1 with IC 50 s of 0.8 nM and 4 nM, respectively. Rebastinib also inhibits SRC, KDR, FLT3, and Tie-2, and has low activity to seen towards c-Kit.

性状

Solid

IC50 & Target[1][2]

IC50: 0.75±0.11 nM (ABL1), 2±0.3 nM (FLT3), 4±0.3 nM (KDR), 6±0.3 nM (TIE2), 34±6 nM (SRC)

体外研究(In Vitro)

Rebastinib potently (IC50 0.82 nM) inhibits u-ABL1, which is thought to exist predominantly in the inactive type II conformation. In addition, Rebastinib also strongly inhibits p-ABL1 (IC50 2 nM), which more readily adopts an active, Type I conformation.
Rebastinib potently inhibits both u-ABL1 (IC50 5 nM) and p-ABL1 (IC50 4 nM), both of which exist predominately in the Type I conformation due to stabilization of an activating hydrophobic spine by the T315I mutation.
In addition to ABL1, Rebastinib also inhibits the SRC family kinases LYN, SRC, FGR, and HCK, and PDGFRα, and PDGFRβ with IC50 of 29±1, 34±6, 38±1, 40±1, 70±10 and 113±10 nM, respectively. Notably, Rebastinib spared c-KIT (IC50 481 nM).
Rebastinib effectively inhibits the proliferation of Ba/F3 cells expressing native BCR-ABL1 (IC

体内研究(In Vivo)

A single dose of Rebastinib (DCC-2036; oral; 100 mg/kg) affords circulating plasma levels that exceeds 12 μM for up to 24 hours, and effectively inhibits BCR-ABL1 signaling for up to 8 hours in Ba/F3-BCR-ABL1 leukemia cells isolated from BM and spleen of tumor-bearing mice.
Treatment of mice bearing Ba/F3-BCR-ABL1 leukemia cells with Rebastinib at 100 mg/kg once daily by oral gavage significantly prolonged their survival, while STI571 at 100 mg/kg twice daily is ineffective.
In this aggressive allograft model, Rebastinib is as effective for treatment of BCR-ABL leukemia as STI571 at 100 mg/kg twice daily in BCR-ABL1 leukemia, and reduces the leukemia cell burden in the spleens of treated mice.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Chan WW, et al. Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell. 2011, 19(4), 556-568.

溶解度数据	In Vitro: DMSO : 50 mg/mL (90.32 mM; ultrasonic and warming and heat to 80°C)配制储备液

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