2. Antibody-drug Conjugate/ADC Related Protein Tyrosine Kinase/RTK Apoptosis Cytoskeleton Cell Cycle/DNA Damage MAPK/ERK Pathway Stem Cell/Wnt PI3K/Akt/mTOR
  3. Antibody-Drug Conjugates (ADCs) c-Kit Apoptosis Microtubule/Tubulin ERK Akt Caspase
  4. NN3201

NN3201 是一种靶向 c-Kit 的抗体-药物偶联物 (ADC)，具有高亲和力 (KD = 0.19 pM)。NN3201 由 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) 和 抗 c-Kit 人源单克隆抗体 NN2101 (HY-P991293) 偶联合成。NN3201 能够快速内化并抑制 SCF 驱动的信号传导，通过递送有效载荷诱导细胞周期阻滞和凋亡 (apoptosis)。由于 FcγR 结合力降低，NN3201 不表现出 Fc 介导的 ADCC 和 CDC 效应功能。NN3201 在多种肿瘤模型中表现出显著的 c-Kit 依赖性抗肿瘤功效。NN3201 可用于小细胞肺癌 (SCLC) 、胃肠道间质瘤 (GIST) 和急性髓系白血病 (AML) 的相关研究[1][2]。

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NN3201

NN3201 Chemical Structure

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NN3201 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NN3201 is a c-Kit-targeting antibody-drug conjugate (ADC) with high affinity (KD = 0.19 pM). NN3201 is composed of 4-(3-Tosyl-2-(tosylmethyl)propanoyl)benzoic acid-glu(PEG24-Me)-val-cit-NH-benzyloxyformic acid-MMAE (HY-178219) and an anti-c-Kit human monoclonal antibody NN2101 (HY-P991293). NN3201 rapidly internalizes and inhibits stem cell factor (SCF)-driven signaling, thereby delivering its payload to induce cell cycle arrest and apoptosis. NN3201 exhibits no Fc-mediated effector functions antibody-dependent cell-mediated cytotoxicity (ADCC)/complement-dependent cytotoxicity (CDC) due to reduced FcγR binding. NN3201 exhibits significant c-Kit-dependent anti-tumor efficacies in various tumor models. NN3201 can be used in small cell lung cancer (SCLC) and gastrointestinal stromal tumor (GIST) and acute myeloid leukemia (AML) research[1][2].

体外研究
(In Vitro)

NN3201 (1 µg/mL，1 小时) 与 c-Kit 高/中表达细胞系表现出剂量依赖性结合，在 315 pM 时达到饱和，未观察到其与 c-Kit 低表达或阴性细胞系结合[1]。
NN3201 (1 µg/mL，0.5-24 小时) 在 c-Kit 阳性的 GIST-T1 细胞中快速 (30 分钟内) 并持续内化，信号在 24 小时内持续增强，且其内化作用依赖于 c-Kit[1]。
NN3201 (3-7 天) 在一组 c-Kit 阳性细胞系中表现出由其 MMAE 有效载荷介导的强效且 c-Kit 依赖性细胞毒性，GI50 值分别为 0.09 nM (GIST-T1)、0.69 nM (GIST-430)、0.12 nM (GIST-430/654) 和 17.06 nM (NCI-H1048)[1]。
NN3201 (0.01-1 µg/mL, 1小时) 剂量依赖性地降低 NCI-H1048 细胞中 SCF 介导的 c-Kit (Y719、Y568/570)、Erk1/2 和 Akt (S473) 的磷酸化，而在 GIST-430/654 细胞中仅部分抑制了 pY568/570 c-Kit 和 pErk1/2 的磷酸化[1]。
NN3201 (1 µg/mL，1-3 天) 通过持续内化诱导 c-Kit 降解和信号抑制，从而引发细胞凋亡，其表现为 caspase-3 和 caspase-7 的裂解增加[1]。
NN3201 (5 µg/mL，24-48 小时) 诱导细胞周期阻滞于 G2/M 期和亚 G1 期，这归因于其释放的 MMAE 有效载荷的微管 (Microtubule/Tubulin) 的破坏作用[1]。
NN3201 (4 µg/mL，7 天) 引发了强烈的旁观者效应，该效应由 NN3201 处理的 GIST-430/654 细胞释放的游离 MMAE 介导，从而导致邻近的 c-Kit 表达水平极低的 MCF7-GFP⁺ 癌细胞死亡[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NN3201 相关抗体:

Cell Viability Assay[1]

Cell Line: MCF7-GFP+ cells
Concentration: 4 μg/mL
Incubation Time: 7 days
Result: Exhibited negligible cytotoxicity (GI50 >20 µg/mL) against the c-Kit-negative MCF7-GFP⁺ cell line, consistent with its target-dependent mechanism and in sharp contrast to the potent activity of its free payload, MMAE (GI50 = 4.96 nM).

Cell Cycle Analysis[1]

Cell Line: GIST-430/654 and NCI-H1048 cells
Concentration: 1 μg/mL
Incubation Time: 24 and 48 h
Result: Induced substantial cell cycle arrest at the G2/M phase and increased the sub-G1 population in both cell lines.

Western Blot Analysis[1]

Cell Line: GIST-430/654 and MCI-H1048 cells
Concentration: 1 μg/mL
Incubation Time: 1, 2, and 3 days
Result: Induced a time-dependent degradation of c-Kit in both cell lines.
Increased levels of cleaved caspase-3 and caspase-7.
Eventually inhibited the c-Kit downstream signaling pathway by sustained internalization and degradation of the NN3201-c-Kit complex over 3 days.
体内研究
(In Vivo)

NN3201 (0.5-10 mg/kg，静脉注射，每 10 天给药一次，共 3 次；或每周给药一次，共 3 次) 在多种胃肠道间质瘤 (GIST) 和小细胞肺癌 (SCLC) 肿瘤小鼠模型中，表现出显著的 c-Kit 依赖性抗肿瘤功效[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female C.B-17 SCID mice (5-6 weeks old) subcutaneously injected with GIST-T1 cells[1]
Dosage: 0.5, 1.5 and 3.0 mg/kg
Administration: i.v., Q10D x 3
Result: Completely regressed tumor volume for up to 112 days at 1.5 and 3 mg/kg, with Imatinib (HY-15463) (100 mg/kg, p.o., Q1D x 30) only inhibited tumor progression during the treatment period.
Induced no body weight loss but rather an increase as tumor size enlarges.
Animal Model: NOG mice (5-6 weeks old) subcutaneously injected with GIST-430/654 cells[1]
Dosage: 1, 3 and 5 mg/kg
Administration: i.v., Q1W x 3
Result: Induced significant tumor shrinkage at 3 mg/kg and 5 mg/kg, and stably controlled until day 42 and 49, respectively.
Induced tumor growth inhibition (TGI) of 47.2 % on day 21 at 1 mg/kg, which was similar to that by 30 mg/kg of Sunitinib (HY-10255A) (30 mg/kg, p.o., Q1D x 21; TGI of 45.2 % on day 21).
Induced no body weight loss but rather an increase as tumor size enlarges.
Animal Model: Female NOD/SCID mice subcutaneously implanted with GS5108 tumors[1]
Dosage: 3, 5 and 10 mg/kg
Administration: i.v., Q1W x 3
Result: Induced durable tumor stasis at 10 mg/kg, which was followed by significant tumor regression for up to 60 days.
Demonstrated superior in vivo efficacy over all standard-of-care (SoC) treatments in the 3rd line GIST models.
Induced no body weight loss but rather an increase as tumor size enlarges.
Animal Model: Female C.B-17 SCID mice (5-6 weeks old) subcutaneously injected with NCI-H526 cells[1]
Dosage: 1, 1.5, 2, 2.5 and 3 mg/kg
Administration: i.v., Q1W x 3
Result: Induced complete regression of the tumor with no regrowth after 70 and 84 days at 2.5 and 3 mg/kg.
Exhibited 84.9 % of TGI compared to the vehicle control on day 17 at 2 mg/kg.
Induced no body weight loss but rather an increase as tumor size enlarges.
Animal Model: Female C.B-17 SCID mice (5-6 weeks old) subcutaneously injected with NCI-H1048 cells[1]
Dosage: 1, 3, and 5 mg/kg
Administration: i.v., Q1W x 3
Result: Showed TGI of 95.1 % on day 21 at 1 mg/kg, better than the combination of Carboplatin (HY-17393) (60 mg/kg, i.p., day 0 and 10) and Etoposide (HY-13629) (3 mg/kg. i.p., day 0~4 and 10~14; TGI = 70.51 % on day 21).
Induced complete tumor remission for up to 35 days and 56 days at 3 mg/kg and 5 mg/kg, respectively.
Induced no body weight loss but rather an increase as tumor size enlarges.
Animal Model: Female C.B-17 SCID mice (5-6 weeks old) subcutaneously injected with NCI-H1048 cells[1]
Dosage: 5 mg/kg
Administration: i.v., Q1W x 3
Result: Was able to reduce the tumor volume to below baseline, whereas neither Topotecan (HY-13768) (0.83 mg/kg, i.p., BIW x 3) nor Irinotecan (HY-16562) (33 mg/kg, i.v., Q1W x 3) could achieve this.
Induced no body weight loss but rather an increase as tumor size enlarges.
Animal Model: Female C.B-17 SCID mice (5-6 weeks old) subcutaneously injected with SHP-77 cells[1]
Dosage: 1, 3, and 5 mg/kg
Administration: i.v., Q1W x 3
Result: Exhibited no in vivo potency in SHP-77 xenografts, where c-Kit expression is negligible, confirming its c-Kit driven property.
Induced no body weight loss but rather an increase as tumor size enlarges.
Animal Model: Female Hsd: Athymic Nude-Foxn1nu mice subcutaneously implanted with CTG-1252 tumors[1]
Dosage: 1, 3, and 5 mg/kg
Administration: i.v., Q1W x 3
Result: Dose-dependently inhibited tumor growth.
Achieved 70 days of complete regression at 5 mg/kg.
Induced no body weight loss but rather an increase as tumor size enlarges.
Animal Model: Female Hsd: Athymic Nude-Foxn1nu mice subcutaneously implanted with CTG-2093 tumors[1]
Dosage: 1, 3, and 5 mg/kg
Administration: i.v., Q1W x 3
Result: Induced tumor stasis until day 27 with TGI of 84.8 % at 5 mg/kg.
Induced no body weight loss but rather an increase as tumor size enlarges.
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.
纯度 & 产品资料
参考文献

NN3201 相关分类

  • 摩尔计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NN3201NN 3201NN-3201Antibody-Drug Conjugates (ADCs)c-KitApoptosisMicrotubule/TubulinERKAktCaspaseAntibody-Drug ConjugatesSCFRCD117Extracellular signal regulated kinasesPKBProtein kinase BADCc-Kit-positive tumorsSCF-driven signalingapoptosisFcγRSCLCGISTNCI-H1048MCF7-GFP?GIST-430/654AMLInhibitorinhibitorinhibit

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