VU0359595(Synonyms: CID-53361951; ML-270)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VU0359595 (Synonyms: CID-53361951; ML-270)

VU0359595 (CID-53361951; ML-270) 是一种选择性磷脂酶 D1 (PLD1) 抑制剂,IC50 值为 3.7 nM。VU0359595 对 PLD1 的选择性比 PLD2 (IC50=6.4 μM) 高 1700 倍以上。VU0359595 可用于癌症、糖尿病、神经退行性疾病和炎性疾病等疾病研究。

VU0359595(Synonyms: CID-53361951;  ML-270)

VU0359595 Chemical Structure

CAS No. : 1246303-14-9

规格 是否有货
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250 mg   询价  
500 mg   询价  

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生物活性

VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases[1][2][3][4].

IC50 & Target[1]

PLD1

3.7 nM (IC50)

PLD2

6.4 μM (IC50)

体外研究
(In Vitro)

VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells[2].
VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2].
VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [3H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells[3].
VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4].
VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

497.43

Formula

C25H29BrN4O2

CAS 号

1246303-14-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009;19(7):1916-1920.

    [2]. Burkhardt U, et al. Phospholipase D is a target for inhibition of astroglial proliferation by ethanol. Neuropharmacology. 2014;79:1-9.

    [3]. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019;184:243-257.

    [4]. Bermúdez V, et al. Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. Front Cell Neurosci. 2019;13:154. Published 2019 Apr 24.

    [5]. Jia X, et al. Gliotoxin promotes Aspergillus fumigatus internalization into type II human pneumocyte A549 cells by inducing host phospholipase D activation. Microbes Infect. 2014 Jun;16(6):491-501.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

VU0359595(Synonyms: CID-53361951; ML-270)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VU0359595 (Synonyms: CID-53361951; ML-270)

VU0359595 (CID-53361951; ML-270) 是一种选择性磷脂酶 D1 (PLD1) 抑制剂,IC50 值为 3.7 nM。VU0359595 对 PLD1 的选择性比 PLD2 (IC50=6.4 μM) 高 1700 倍以上。VU0359595 可用于癌症、糖尿病、神经退行性疾病和炎性疾病等疾病研究。

VU0359595(Synonyms: CID-53361951;  ML-270)

VU0359595 Chemical Structure

CAS No. : 1246303-14-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases[1][2][3][4].

IC50 & Target[1]

PLD1

3.7 nM (IC50)

PLD2

6.4 μM (IC50)

体外研究
(In Vitro)

VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells[2].
VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2].
VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [3H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells[3].
VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4].
VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

497.43

Formula

C25H29BrN4O2

CAS 号

1246303-14-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009;19(7):1916-1920.

    [2]. Burkhardt U, et al. Phospholipase D is a target for inhibition of astroglial proliferation by ethanol. Neuropharmacology. 2014;79:1-9.

    [3]. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019;184:243-257.

    [4]. Bermúdez V, et al. Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. Front Cell Neurosci. 2019;13:154. Published 2019 Apr 24.

    [5]. Jia X, et al. Gliotoxin promotes Aspergillus fumigatus internalization into type II human pneumocyte A549 cells by inducing host phospholipase D activation. Microbes Infect. 2014 Jun;16(6):491-501.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

VU0359595(Synonyms: CID-53361951; ML-270)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VU0359595 (Synonyms: CID-53361951; ML-270)

VU0359595 (CID-53361951; ML-270) 是一种选择性磷脂酶 D1 (PLD1) 抑制剂,IC50 值为 3.7 nM。VU0359595 对 PLD1 的选择性比 PLD2 (IC50=6.4 μM) 高 1700 倍以上。VU0359595 可用于癌症、糖尿病、神经退行性疾病和炎性疾病等疾病研究。

VU0359595(Synonyms: CID-53361951;  ML-270)

VU0359595 Chemical Structure

CAS No. : 1246303-14-9

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

VU0359595 (CID-53361951; ML-270) is a potent and selective pharmacological phospholipase D1 (PLD1) inhibitor with an IC50 of 3.7 nM. VU0359595 is >1700-fold selective for PLD1 over PLD2 (IC50 of 6.4 μM). VU0359595 can be used for the research of cancer, diabetes, neurodegenerative and inflammatory diseases[1][2][3][4].

IC50 & Target[1]

PLD1

3.7 nM (IC50)

PLD2

6.4 μM (IC50)

体外研究
(In Vitro)

VU0359595 (5, 50, 500, 5000 nM) inhibits basal and FCS/IGF-1 stimulated proliferation of astroglial cells[2].
VU0359595 (5, 50, 500 nM; 30 min) does not affect basal PLD activity in astrocytes but reduces mitogen-stimulated PLD activity in a concentration-dependent manner[2].
VU0359595 (0.15 μM; 1 h before high glucose treatment and 4 h during high glucose treatment) partially reduces the increase [3H]-phosphatidylethanol (PEth) generation induced by high glucose (33 mM) in retinal pigment epithelium (RPE) cells[3].
VU0359595 (5 μM; 1 h prior to LPS treatment) modulates the autophagic process of LPS-induced (10 μg/ml; 24 h) RPE cells[4].
VU0359595 (2 nM; pretreatment 30 min) blocks the increase of A. fumigatus internalization induced by 50 ng/ml gliotoxin in A549 cells[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

497.43

Formula

C25H29BrN4O2

CAS 号

1246303-14-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009;19(7):1916-1920.

    [2]. Burkhardt U, et al. Phospholipase D is a target for inhibition of astroglial proliferation by ethanol. Neuropharmacology. 2014;79:1-9.

    [3]. Tenconi PE, et al. High glucose-induced phospholipase D activity in retinal pigment epithelium cells: New insights into the molecular mechanisms of diabetic retinopathy. Exp Eye Res. 2019;184:243-257.

    [4]. Bermúdez V, et al. Lipopolysaccharide-Induced Autophagy Mediates Retinal Pigment Epithelium Cells Survival. Modulation by the Phospholipase D Pathway. Front Cell Neurosci. 2019;13:154. Published 2019 Apr 24.

    [5]. Jia X, et al. Gliotoxin promotes Aspergillus fumigatus internalization into type II human pneumocyte A549 cells by inducing host phospholipase D activation. Microbes Infect. 2014 Jun;16(6):491-501.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

VU0469650

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VU0469650 

VU0469650 是一种有效的、选择性的、穿透 CNS 的 mGlu1 受体的反向变构调节剂,其 IC50 为99 nM。

VU0469650

VU0469650 Chemical Structure

CAS No. : 1443748-47-7

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

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生物活性

VU0469650 is a potent, selective and CNS-penetrated negative allosteric modulator of mGlu1 receptor, with an IC50 of 99 nM[1].

IC50 & Target

mGluR 1

99 nM (IC50)

体内研究
(In Vivo)

VU0469650 (male Sprague-Dawley rats, 0.2 mg/kg, IV, once) exhibits moderate to high clearance, a moderate volume of distribution, and a half-life of approximately 1 hour[1].
VU0469650 (male Sprague-Dawley rats, 10 mg/kg, IP, once) shows an excellent selectivity profile and good exposure in both plasma and brain samples[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

364.48

Formula

C22H28N4O

CAS 号

1443748-47-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Lovell KM, Felts AS, Rodriguez AL, et al. N-Acyl-N’-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013;23(13):3713-3718.

Animal Administration

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Lovell KM, Felts AS, Rodriguez AL, et al. N-Acyl-N’-arylpiperazines as negative allosteric modulators of mGlu1: identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg Med Chem Lett. 2013;23(13):3713-3718.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

VU0155069(Synonyms: CAY10593)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VU0155069 (Synonyms: CAY10593)

VU0155069 (CAY10593),化合物 69 是一种选择性磷脂酶 D1 (PLD1) 抑制剂,IC50 值为 46 nM。VU0155069 (CAY10593) 在 transwell 测定中强烈抑制几种癌细胞系的侵袭性迁移。

VU0155069(Synonyms: CAY10593)

VU0155069 Chemical Structure

CAS No. : 1130067-06-9

规格 是否有货
5 mg 询价

* Please select Quantity before adding items.

生物活性

VU0155069 (CAY10593), compound 69, is a selective phospholipase D1 (PLD1) inhibitor with an IC50 value of 46 nM in vitro[1]. VU0155069 (CAY10593) strongly inhibits the invasive migration of several cancer cell lines in transwell assays[2].

IC50 & Target

PLD1

46 nM (IC50)

PLD2

933 nM (IC50)

分子量

462.97

Formula

C26H27ClN4O2

CAS 号

1130067-06-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Scott SA, et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat Chem Biol. 2009 Feb;5(2):108-17.

    [2]. Lewis JA, et al. Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part I: Impact of alternative halogenated privileged structures for PLD1 specificity. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1916-20.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

VU0661013

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VU0661013  纯度: 98.52%

VU661013 是一种有效的选择性 MCL-1 抑制剂。

VU0661013

VU0661013 Chemical Structure

CAS No. : 2131184-57-9

规格 价格 是否有货 数量
5 mg ¥5500 In-stock
10 mg ¥8500 In-stock
25 mg ¥17500 In-stock
50 mg ¥27500 In-stock
100 mg ¥39500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

VU0661013 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • Anti-Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

VU661013 is a potent and selective MCL-1 inhibitor.

IC50 & Target

Mcl-1

 

体外研究
(In Vitro)

VU661013 exhibits a Ki of 97±30 pM to human MCL-1 in a TR-FRET assay by displacing a fluorescently labeled peptide derived from the pro-apoptotic protein BAK. However, VU661013 does not significantly inhibit BCL-xL (Ki>40 μM) or BCL-2 (Ki=0.73 μM)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

VU661013, a novel, potent, selective MCL-1 inhibitor that de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML, and is active in Venetoclax-resistant cells and patient derived xenografts. After establishing disseminated leukemia, NSGS mice are dosed intraperitoneally with 10, 25 or 75 mg/kg of VU661013 daily for 21 days. Weekly chimerism analyses are conducted and the percentage of MV-4-11 cells are quantified in murine peripheral blood using anti-human CD45 (hCD45) and anti-hCD33 monoclonal antibodies. Twenty-eight days post-transplant, vehicle-treated mice have developed large leukemia burdens and thus, mice are sacrificed, and their organs are harvested for analysis. Vehicle mice treated died of xenografted AML, but have no evidence of VU661013-related toxicity in non target organs. VU661013 treatment of disseminated human AML results in a dose-dependent decrease in tumor burden, nearly eliminating the hCD45+ MV-4-11 cells at the 75 mg/kg dose in the blood (mean, 13.0±2.2% in vehicle vs 7.4±7.2% in 25mg/kg vs 0.17±0.12% in 75 mg/kg treated mice), bone marrow (mean, 40.7±13.9% in vehicle vs 33.46±4.0 % in 25 mg/kg vs 0.384±0.345 in 75 mg/kg treated mice), and spleen (mean, 46.22±13.3% in vehicle vs 13.31±10.0% in 25 mg/kg vs 1.588±1.51% in 75 mg/kg treated mice). Treatment with VU661013 reduces disease-associated splenomegaly (mean, vehicle vs. 75mg/kg, 0.17±0.02 vs 0.09±0.01g), and amendeding spleen to body weight ratio (vehicle vs 75mg/kg, 0.99 vs 0.50). In a second MV-4-11 xenograft study, mice are followed until death, and survival is evaluated by Kaplan-Meier analysis. In this study, NSGS mice are treated daily (starting 7 days after transplant) with vehicle only, 15 mg/kg or 75 mg/kg of VU661013. Analysis reveals an increase in survival in mice treated with the 75mg/kg dose (vehicle treated mice=31 days, vs 15 mg/kg=32 days, vs 75 mg/kg treated mice=43 Days)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

712.66

Formula

C39H39Cl2N5O4

CAS 号

2131184-57-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 125 mg/mL (175.40 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.4032 mL 7.0160 mL 14.0319 mL
5 mM 0.2806 mL 1.4032 mL 2.8064 mL
10 mM 0.1403 mL 0.7016 mL 1.4032 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.92 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.92 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (2.92 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (2.92 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Haley E. Ramsey, et al. A Novel MCL-1 Inhibitor Combined with Venetoclax Rescues Venetoclax Resistant Acute Myelogenous Leukemia. Cancer Discov. August 28, 2018.

Cell Assay
[1]

To generate cells that are resistant to BCL-2 or MCL-1 inhibition, MV-4-11 cells are treated over the course of 3 months with gradually increasing concentrations of VEN (5 nM to 2.5 μM) or VU661013 (100 nM to 5 μM). Cells are declared to be VEN or VU661013-resistant when they are able to maintain 100% viability in the presence of these high concentrations (5 μM of VU661013 and 2.5 μM of VEN) of inhibitors[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]
Upon establishing microchimerism, mice are treated with either Venetoclax by daily gavage, VU661013 (10, 25 or 75 mg/kg) by daily i.p injection, or vehicle. VU661013 is dissolved in DMSO and diluted in ethanol, Polyethylene Glycol (PEG), and saline. Venetoclax is dissolved in PEG and ethanol, and diluted with Phosal 50 PG. Peripheral blood is assessed weekly for human chimerism. Spleen/body ratio is calculated as organ weight (gram) per gram of body weight[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Haley E. Ramsey, et al. A Novel MCL-1 Inhibitor Combined with Venetoclax Rescues Venetoclax Resistant Acute Myelogenous Leukemia. Cancer Discov. August 28, 2018.

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