MRTX-EX185

发表于2024年4月13日由上海金畔生物科技有限公司

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。

MRTX-EX185

MRTX-EX185 是负载 GDP 的 KRAS 和 KRAS(G12D) 的有效抑制剂，对 KRAS(G12D) 的 IC₅₀ 值为 90 nM。MRTX-EX185 还结合 GDP 负载的 HRAS。

MRTX-EX185 Chemical Structure

规格	价格	是否有货
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10 mg	￥20500	询问价格 & 货期

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生物活性	MRTX-EX185 is a potent inhibitor of GDP-loaded KRAS and KRAS(G12D), with an IC₅₀ of 90 nM for KRAS(G12D). MRTX-EX185 also binds GDP-loaded HRAS^[1].
分子量	564.65
Formula	C₃₃H₃₃FN₆O₂
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]. Vasta JD, et, al. KRAS is vulnerable to reversible switch-II pocket engagement in cells. Nat Chem Biol. 2022 Mar 21.

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MRTX1133 formic

发表于2024年4月10日由上海金畔生物科技有限公司

MRTX1133 formic

MRTX1133 formic 是一种非共价、强效和选择性 KRAS G12D 抑制剂。MRTX1133 formic 以最佳方式填充开关 II 口袋，并延伸三个取代基以与蛋白质良好地相互作用，对 KRAS G12D 的 K_D 为 0.2 pM。MRTX1133 formic 阻止 SOS1 催化的核苷酸交换和/或KRAS G12D/GTP/RAF1 复合物的形成，从而抑制突变体 KRAS 依赖性信号转导。MRTX1133 formic 具有皮摩尔结合亲和力，在细胞实验中具有一位数纳摩尔活性，在含有 KRAS G12D 突变的肿瘤模型中具有显著的体内疗效。

MRTX1133 formic Chemical Structure

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5 mg	￥5100	询问价格 & 货期
10 mg	￥8200	询问价格 & 货期
25 mg	￥16400	询问价格 & 货期
50 mg	￥26200	询问价格 & 货期

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MRTX1133 formic 的其他形式现货产品:

MRTX1133

生物活性

MRTX1133 formic is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 formic optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D against KRAS G12D of 0.2 pM. MRTX1133 formic prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRASG12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 formic has picomolar binding affinity, single digit nanomolar activity in cellular assays, and marked in vivo efficacy in tumor models harboring KRAS G12D mutations^[1]^[2].

IC₅₀ & Target^[1]

KRas G12D

0.2 pM (Kd)

体外研究
(In Vitro)

MRTX1133 formic inhibits ERK phosphorylation in the AGS cell line with an IC₅₀ ranging 1-10 nM (AsPC-1, Panc 04.03, Panc 02.03, SW1990, GP2D, Suit2, A427, SNU1033, and HPAC cells). In a 2D viability assay, the IC₅₀ of MRTX1133 formic is 6 nM against AGS cells (KRAS G12D), while demonstrating more than 500-fold selectivity against MKN1, a cell line which is dependent on KRAS for its growth and survival due to the amplification of wild-type KRAS^[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)

MRTX1133 demonstrates dose-dependent inhibition of the KRAS pathway tumor regression in G12D mutant tumor models^[2].

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

646.66

Formula

C₃₄H₃₃F₃N₆O₄

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 50 mg/mL (77.32 mM; Need ultrasonic)

H₂O : 25 mg/mL (38.66 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5464 mL	7.7320 mL	15.4641 mL
5 mM	0.3093 mL	1.5464 mL	3.0928 mL
10 mM	0.1546 mL	0.7732 mL	1.5464 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 (sealed storage, away from moisture)。-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 (3.22 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.22 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 (3.22 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.22 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 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

*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]. Wang X, et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor [published online ahead of print, 2021 Dec 10]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01688.

[2]. KRAS G12D Inhibitor: MRTX1133. [(accessed on 22 April 2021)];2021 Available online.

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ASP2453

发表于2024年2月26日由上海金畔生物科技有限公司

ASP2453

ASP2453是一种强效、选择性和共价的KRAS G12C抑制剂。ASP2453抑制Son of Sevenless (SOS)介导的KRAS G12C和Raf之间的相互作用，IC₅₀值为40 nM。

ASP2453 Chemical Structure

CAS No. : 2241719-73-1

规格	价格	是否有货
5 mg	￥8500	询问价格 & 货期
10 mg	￥14500	询问价格 & 货期

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生物活性

ASP2453 is a potent, selective and covalent KRAS G12C inhibitor. ASP2453 inhibits the Son of Sevenless (SOS)-mediated interaction between KRAS G12C and Raf with an IC₅₀ value of 40 nM.

IC₅₀ & Target

KRas G12C

40 nM (IC₅₀)

分子量

747.85

Formula

C₄₀H₄₈F₃N₇O₄

CAS 号

2241719-73-1

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]. Nakayama A, et al. Characterisation of a novel KRAS G12C inhibitor ASP2453 that shows potent anti-tumour activity in KRAS G12C-mutated preclinical models. Br J Cancer. 2021 Nov 18.

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PROTAC KRAS G12C degrader-1

发表于2024年2月23日由上海金畔生物科技有限公司

PROTAC KRAS G12C degrader-1

PROTAC KRAS G12C degrader-1 是一种基于 Cereblon 的 KRAS^G12C 降解剂，对 CRBN 的 IC₅₀ 为 414 nM。PROTAC KRAS G12C degrader-1 诱导 CRBN/KRAS^G12C 二聚化并降解报告细胞中的 GFP-KRAS^G12C。

PROTAC KRAS G12C degrader-1 Chemical Structure

规格	价格	是否有货
5 mg	￥12800	询问价格 & 货期
10 mg	￥20500	询问价格 & 货期

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生物活性	PROTAC KRAS G12C degrader-1 is a Cereblon-based KRAS^G12C degrader, with an IC₅₀ of 414 nM for CRBN. PROTAC KRAS G12C degrader-1 induces CRBN/ KRAS^G12C dimerization and degrades GFP- KRAS^G12C in reporter cells^[1].
体外研究 (In Vitro)	PROTAC KRAS G12C degrader-1 (Compound 12) engages CRBN in cells, bound KRASG12C in vitro, induces CRBN/KRASG12C dimerization, and degrades GFP-KRASG12C in reporter cells in a CRBN-dependent manner^[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	917.47
Formula	C₅₀H₅₄ClFN₈O₆
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]. Zeng M, et, al. Exploring Targeted Degradation Strategy for Oncogenic KRAS G12C. Cell Chem Biol. 2020 Jan 16;27(1):19-31.e6.

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KRA-533

发表于2024年2月15日由上海金畔生物科技有限公司

KRA-533

KRA-533 是一种有效的 KRAS 激动剂。KRA-533 与 KRAS 蛋白中的 GTP/GDP binding pocket 结合，防止 GTP 切割，导致 GTP 结合 KRAS 的组成性活性积累，触发癌细胞中凋亡和自噬细胞死亡途径。

KRA-533 Chemical Structure

CAS No. : 10161-87-2

规格	价格	是否有货
5 mg	￥2800	询问价格 & 货期
10 mg	￥4200	询问价格 & 货期
25 mg	￥8000	询问价格 & 货期
50 mg	￥11900	询问价格 & 货期

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生物活性

KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

IC₅₀ & Target

KRAS^[1]

体外研究
(In Vitro)

KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent^[1].
KRA-533 (0~15 μM; 48 hours; H157 cells) enhances KRAS activity in a dose-dependent manner, which is associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death^[1].
KRA-533 (10 μM; 10 days; H292 cells) mediates cell growth suppression than those without KRAS mutation. KRA-533 (5~15 μM) can directly bind to WT, G12C, G12D and G13D mutant KRAS proteins. KRA-533 activates WT KRAS to increase its activity in a dose-dependent manner. KRA-533 further enhances the activities of active KRAS mutants^[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.

Western Blot Analysis^[1]

Cell Line:	HCC827 cells
Concentration:	10 μM
Incubation Time:	48 hours
Result:	Enhanced KRAS activity to a greater extent.

Apoptosis Analysis^[1]

Cell Line:	H157 cells
Concentration:	0~15 μM
Incubation Time:	48 hours
Result:	Enhanced KRAS activity in a dose-dependent manner, which was associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death.

体内研究
(In Vivo)

KRA-533 (0~30 mg/kg; 28 days) suppresses tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induces apoptosis and autophagy in tumor tissues in a dose-dependent manner^[1].
KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses^[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 Model:	Nu/Nu nude mice^[1]
Dosage:	0~30 mg/kg
Administration:	I.p.
Result:	Suppressed tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induced apoptosis and autophagy in tumor tissues in a dose-dependent manner.

分子量

314.18

Formula

C₁₃H₁₆BrNO₃

CAS 号

10161-87-2

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

参考文献

[1]. Xu K, et al. Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy [published correction appears in Mol Cancer. 2020 May 20;19(1):93]. Mol Cancer. 2019;18(1):85. Published 2019 Apr 10.

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KRAS G13D peptide, 25 mer

发表于2024年1月21日由上海金畔生物科技有限公司

KRAS G13D peptide, 25 mer

KRAS G13D peptide, 25 mer，KRAS 激活癌基因突变肽，是一种免疫增强剂。KRAS G13D peptide, 25 mer 可用于制备 KRAS 疫苗。详细信息请参考专利文献 WO2018144775A1。

KRAS G13D peptide, 25 mer Chemical Structure

CAS No. : 145019-94-9

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100 mg		询价
250 mg		询价
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生物活性	KRAS G13D peptide, 25 mer, a KRAS activating oncogene mutation peptide, is an immune potentiator extracted from patent WO2018144775A1. KRAS G13D peptide, 25 mer can be used to prepare KRAS vaccine^[1].
体外研究 (In Vitro)	KRAS G13D peptide, 25 mer is encoded by immunomodulatory therapeutic mRNA that can be used to prepare KRAS vaccine^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	2634.10
Formula	C_{1₁₈H₂₀1}N₂₉O₃₆S
CAS 号	145019-94-9
Sequence	Met-Thr-Glu-Tyr-Lys-Leu-Val-Val-Val-Gly-Ala-Gly-Asp-Val-Gly-Lys-Ser-Ala-Leu-Thr-Ile-Gln-Leu-Ile-Gln
Sequence Shortening	MTEYKLVVVGAGDVGKSALTIQLIQ
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]. Huang EYC, et, al. Immunomodulatory therapeutic mrna compositions encoding activating oncogene mutation peptides. WO2018144775A1.

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KRAS G13D peptide, 25 mer

发表于2024年1月21日由上海金畔生物科技有限公司

KRAS G13D peptide, 25 mer

KRAS G13D peptide, 25 mer，KRAS 激活癌基因突变肽，是一种免疫增强剂。KRAS G13D peptide, 25 mer 可用于制备 KRAS 疫苗。详细信息请参考专利文献 WO2018144775A1。

KRAS G13D peptide, 25 mer Chemical Structure

CAS No. : 145019-94-9

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	KRAS G13D peptide, 25 mer, a KRAS activating oncogene mutation peptide, is an immune potentiator extracted from patent WO2018144775A1. KRAS G13D peptide, 25 mer can be used to prepare KRAS vaccine^[1].
体外研究 (In Vitro)	KRAS G13D peptide, 25 mer is encoded by immunomodulatory therapeutic mRNA that can be used to prepare KRAS vaccine^[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	2634.10
Formula	C_{1₁₈H₂₀1}N₂₉O₃₆S
CAS 号	145019-94-9
Sequence	Met-Thr-Glu-Tyr-Lys-Leu-Val-Val-Val-Gly-Ala-Gly-Asp-Val-Gly-Lys-Ser-Ala-Leu-Thr-Ile-Gln-Leu-Ile-Gln
Sequence Shortening	MTEYKLVVVGAGDVGKSALTIQLIQ
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]. Huang EYC, et, al. Immunomodulatory therapeutic mrna compositions encoding activating oncogene mutation peptides. WO2018144775A1.

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KRAS G13D peptide, 25 mer

发表于2024年1月21日由上海金畔生物科技有限公司

KRAS G13D peptide, 25 mer

KRAS G13D peptide, 25 mer，KRAS 激活癌基因突变肽，是一种免疫增强剂。KRAS G13D peptide, 25 mer 可用于制备 KRAS 疫苗。详细信息请参考专利文献 WO2018144775A1。

KRAS G13D peptide, 25 mer Chemical Structure

CAS No. : 145019-94-9

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	KRAS G13D peptide, 25 mer, a KRAS activating oncogene mutation peptide, is an immune potentiator extracted from patent WO2018144775A1. KRAS G13D peptide, 25 mer can be used to prepare KRAS vaccine^[1].
体外研究 (In Vitro)	KRAS G13D peptide, 25 mer is encoded by immunomodulatory therapeutic mRNA that can be used to prepare KRAS vaccine^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	2634.10
Formula	C_{1₁₈H₂₀1}N₂₉O₃₆S
CAS 号	145019-94-9
Sequence	Met-Thr-Glu-Tyr-Lys-Leu-Val-Val-Val-Gly-Ala-Gly-Asp-Val-Gly-Lys-Ser-Ala-Leu-Thr-Ile-Gln-Leu-Ile-Gln
Sequence Shortening	MTEYKLVVVGAGDVGKSALTIQLIQ
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]. Huang EYC, et, al. Immunomodulatory therapeutic mrna compositions encoding activating oncogene mutation peptides. WO2018144775A1.

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SAH-SOS1A

发表于2024年1月20日由上海金畔生物科技有限公司

SAH-SOS1A

SAH-SOS1A 是一种基于肽的 SOS1/KRAS 蛋白相互作用抑制剂。SAH-SOS1A 以纳摩尔亲和力 (EC₅₀=106-175 nM) 与野生型和突变型 KRAS (G12D, G12V, G12C, G12S, and Q61H) 结合，直接和独立地阻断核苷酸结合，损害 KRAS 驱动的癌细胞活力，并通过阻断 KRAS 下游 ERK-MAPK 磷酸化信号级联的机制发挥作用。

SAH-SOS1A Chemical Structure

CAS No. : 1652561-87-9

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

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SAH-SOS1A 的其他形式现货产品:

SAH-SOS1A TFA

生物活性

SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC₅₀=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS^[1].

IC₅₀ & Target^[1]

KRAS-SOS1

KRas G12C

140 nM (EC₅₀)

KRas G12D

109 nM (EC₅₀)

KRas G12V

154 nM (EC₅₀)

KRas G12S

155 nM (EC₅₀)

KRas Q61H

175 nM (EC₅₀)

K-Ras WT

106 nM (EC₅₀)

体外研究
(In Vitro)

SAH-SOS1A (0.625-40 μM) dose-responsively impairs the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations with IC50 values in the 5- to 15-μM range. Cancer cells expressing wild-type KRAS, such as HeLa and Colo320-HSR cells, are similarly affected^[1].
SAH-SOS1A (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation^[1].

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

Cell Viability Assay^[1]

Cell Line:	Panc 10.05 cells bearing the KRAS G12D mutation
Concentration:	0.625-40 μM
Incubation Time:	24 hours
Result:	Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.

Western Blot Analysis^[1]

Cell Line:	Panc 10.05 cells
Concentration:	5-40 μM
Incubation Time:	Indicated doses for 4 h, followed by 15-min stimulation with EGF
Result:	Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.

体内研究
(In Vivo)

SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85D^V12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2^[1].

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

分子量

2187.53

Formula

C₁₀₀H₁₅₉N₂₇O₂₈

CAS 号

1652561-87-9

Sequence Shortening

RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)

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]. Leshchiner ES, et al. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A. 2015;112(6):1761-1766.

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SAH-SOS1A

发表于2024年1月19日由上海金畔生物科技有限公司

SAH-SOS1A

SAH-SOS1A Chemical Structure

CAS No. : 1652561-87-9

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

* Please select Quantity before adding items.

SAH-SOS1A 的其他形式现货产品:

SAH-SOS1A TFA

生物活性

IC₅₀ & Target^[1]

KRAS-SOS1

KRas G12C

140 nM (EC₅₀)

KRas G12D

109 nM (EC₅₀)

KRas G12V

154 nM (EC₅₀)

KRas G12S

155 nM (EC₅₀)

KRas Q61H

175 nM (EC₅₀)

K-Ras WT

106 nM (EC₅₀)

体外研究
(In Vitro)

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.

Cell Viability Assay^[1]

Cell Line:	Panc 10.05 cells bearing the KRAS G12D mutation
Concentration:	0.625-40 μM
Incubation Time:	24 hours
Result:	Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.

Western Blot Analysis^[1]

Cell Line:	Panc 10.05 cells
Concentration:	5-40 μM
Incubation Time:	Indicated doses for 4 h, followed by 15-min stimulation with EGF
Result:	Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.

体内研究
(In Vivo)

SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85D^V12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2^[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

2187.53

Formula

C₁₀₀H₁₅₉N₂₇O₂₈

CAS 号

1652561-87-9

Sequence Shortening

RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)

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]. Leshchiner ES, et al. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A. 2015;112(6):1761-1766.

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

SAH-SOS1A

发表于2024年1月19日由上海金畔生物科技有限公司

SAH-SOS1A

SAH-SOS1A Chemical Structure

CAS No. : 1652561-87-9

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

* Please select Quantity before adding items.

SAH-SOS1A 的其他形式现货产品:

SAH-SOS1A TFA

生物活性

IC₅₀ & Target^[1]

KRAS-SOS1

KRas G12C

140 nM (EC₅₀)

KRas G12D

109 nM (EC₅₀)

KRas G12V

154 nM (EC₅₀)

KRas G12S

155 nM (EC₅₀)

KRas Q61H

175 nM (EC₅₀)

K-Ras WT

106 nM (EC₅₀)

体外研究
(In Vitro)

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

Cell Viability Assay^[1]

Cell Line:	Panc 10.05 cells bearing the KRAS G12D mutation
Concentration:	0.625-40 μM
Incubation Time:	24 hours
Result:	Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.

Western Blot Analysis^[1]

Cell Line:	Panc 10.05 cells
Concentration:	5-40 μM
Incubation Time:	Indicated doses for 4 h, followed by 15-min stimulation with EGF
Result:	Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.

体内研究
(In Vivo)

SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85D^V12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2^[1].

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

分子量

2187.53

Formula

C₁₀₀H₁₅₉N₂₇O₂₈

CAS 号

1652561-87-9

Sequence Shortening

RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)

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]. Leshchiner ES, et al. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A. 2015;112(6):1761-1766.

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

KRAS G12D inhibitor 15

发表于2023年12月19日由上海金畔生物科技有限公司

KRAS G12D inhibitor 15

KRAS G12D inhibitor 15 是一种有效的 KRAS G12D 抑制剂。KRAS G12D inhibitor 15 具有研究各种疾病或病症的潜力，例如癌症或癌症转移 (摘自专利 WO2022042630A1，化合物 243)。

KRAS G12D inhibitor 15 Chemical Structure

CAS No. : 2763155-39-9

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	KRAS G12D inhibitor 15 is a potent inhibitor of KRAS G12D. KRAS G12D inhibitor 15 has the potential for the research of various diseases or disorders, such as cancer or cancer metastasis (extracted from patent WO2022042630A1, compound 243)^[1].
分子量	924.17
Formula	C₅₃H₇₁F₂N₇O₅
CAS 号	2763155-39-9
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]. Xing DAI, et al. Heteroaryl compounds, preparation methods and uses thereof. Patent WO2022042630A1.

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

KRAS G12D inhibitor 6

发表于2023年12月13日由上海金畔生物科技有限公司

KRAS G12D inhibitor 6

KRAS G12D inhibitor 6 是 KRAS G12D 的有效抑制剂 (信息来自专利 WO2021108683A1，compound 112)。

KRAS G12D inhibitor 6 Chemical Structure

CAS No. : 2648552-32-1

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	KRAS G12D inhibitor 6 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683A1, compound 112) ^[1].
IC₅₀ & Target	KRAS G12D^[1]
分子量	601.14
Formula	C₃₂H₃₇ClN₈O₂
CAS 号	2648552-32-1
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]. PITZEN, Jennifer, et al. COVALENT RAS INHIBITORS AND USES THEREOF. Patent WO2021108683A1.

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

KRAS G12D inhibitor 7

发表于2023年12月13日由上海金畔生物科技有限公司

KRAS G12D inhibitor 7

KRAS G12D inhibitor 7 是 KRAS G12D 的有效抑制剂 (信息来自专利 WO2021108683，compound 114)。

KRAS G12D inhibitor 7 Chemical Structure

CAS No. : 2648552-34-3

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

KRAS G12D inhibitor 7 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683, compound 114) ^[1].

IC₅₀ & Target

KRas G12D

分子量

582.70

Formula

C₃₂H₃₈N₈O₃

CAS 号

2648552-34-3

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]. PITZEN, Jennifer, et al. COVALENT RAS INHIBITORS AND USES THEREOF. Patent WO2021108683A1.

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

KRAS G12D inhibitor 6

发表于2023年12月13日由上海金畔生物科技有限公司

KRAS G12D inhibitor 6

KRAS G12D inhibitor 6 是 KRAS G12D 的有效抑制剂 (信息来自专利 WO2021108683A1，compound 112)。

KRAS G12D inhibitor 6 Chemical Structure

CAS No. : 2648552-32-1

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	KRAS G12D inhibitor 6 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683A1, compound 112) ^[1].
IC₅₀ & Target	KRAS G12D^[1]
分子量	601.14
Formula	C₃₂H₃₇ClN₈O₂
CAS 号	2648552-32-1
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]. PITZEN, Jennifer, et al. COVALENT RAS INHIBITORS AND USES THEREOF. Patent WO2021108683A1.

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

KRAS G12D inhibitor 7

发表于2023年12月13日由上海金畔生物科技有限公司

KRAS G12D inhibitor 7

KRAS G12D inhibitor 7 是 KRAS G12D 的有效抑制剂 (信息来自专利 WO2021108683，compound 114)。

KRAS G12D inhibitor 7 Chemical Structure

CAS No. : 2648552-34-3

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

KRAS G12D inhibitor 7 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683, compound 114) ^[1].

IC₅₀ & Target

KRas G12D

分子量

582.70

Formula

C₃₂H₃₈N₈O₃

CAS 号

2648552-34-3

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]. PITZEN, Jennifer, et al. COVALENT RAS INHIBITORS AND USES THEREOF. Patent WO2021108683A1.

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

KRAS G12D inhibitor 6

发表于2023年12月13日由上海金畔生物科技有限公司

KRAS G12D inhibitor 6

KRAS G12D inhibitor 6 是 KRAS G12D 的有效抑制剂 (信息来自专利 WO2021108683A1，compound 112)。

KRAS G12D inhibitor 6 Chemical Structure

CAS No. : 2648552-32-1

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	KRAS G12D inhibitor 6 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683A1, compound 112) ^[1].
IC₅₀ & Target	KRAS G12D^[1]
分子量	601.14
Formula	C₃₂H₃₇ClN₈O₂
CAS 号	2648552-32-1
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]. PITZEN, Jennifer, et al. COVALENT RAS INHIBITORS AND USES THEREOF. Patent WO2021108683A1.

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

KRAS G12D inhibitor 7

发表于2023年12月13日由上海金畔生物科技有限公司

KRAS G12D inhibitor 7

KRAS G12D inhibitor 7 是 KRAS G12D 的有效抑制剂 (信息来自专利 WO2021108683，compound 114)。

KRAS G12D inhibitor 7 Chemical Structure

CAS No. : 2648552-34-3

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

KRAS G12D inhibitor 7 is a potent inhibitor of KRAS G12D (extracted from patent WO2021108683, compound 114) ^[1].

IC₅₀ & Target

KRas G12D

分子量

582.70

Formula

C₃₂H₃₈N₈O₃

CAS 号

2648552-34-3

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]. PITZEN, Jennifer, et al. COVALENT RAS INHIBITORS AND USES THEREOF. Patent WO2021108683A1.

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

KRAS inhibitor-14

发表于2023年12月10日由上海金畔生物科技有限公司

KRAS inhibitor-14

KRAS inhibitor-14 (compound 3-22) 是一种有效的 KRAS G12C 抑制剂，IC₅₀ 为 0.249 µM。KRAS inhibitor-14 在 MIA PaCA-2，A549 细胞中显示出 p-ERK 抑制活性，IC₅₀s 分别为 1.12，>33.3 µM。KRAS inhibitor-14 具有研究胰腺癌，结直肠癌和肺癌的潜力。

KRAS inhibitor-14 Chemical Structure

CAS No. : 2230873-78-4

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

KRAS inhibitor-14 (compound 3-22) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.249 µM. KRAS inhibitor-14 shows p-ERK inhibition activities with IC₅₀s of 1.12, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-14 has the potential for the research of pancreatic, colorectal, and lung cancers^[1].

IC₅₀ & Target^[1]

KRas G12C

0.249 μM (IC₅₀)

分子量

486.77

Formula

C₂₀H₁₅Cl₃FN₃O₂S

CAS 号

2230873-78-4

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]. Brian alan, et al. KRAS g12c inhibitors and methods of using the same. WO2018119183 A2

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KRAS inhibitor-16

发表于2023年12月10日由上海金畔生物科技有限公司

KRAS inhibitor-16

KRAS inhibitor-16 (compound 3-11) 是一种有效的 KRAS G12C 抑制剂，IC₅₀ 为 0.457 µM。KRAS inhibitor-16 在 MIA PaCA-2，A549 细胞中显示出 p-ERK 抑制活性，IC₅₀s 分别为 3.06，11.1 µM。 KRAS inhibitor-16 具有研究胰腺癌，结直肠癌和肺癌的潜力。

KRAS inhibitor-16 Chemical Structure

CAS No. : 2230873-67-1

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

KRAS inhibitor-16 (compound 3-11) is a potent KRAS G12C inhibitor with an IC₅₀ of 0.457 µM. KRAS inhibitor-16 shows p-ERK inhibition activities with IC₅₀s of 3.06, 11.1 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-16 has the potential for the research of pancreatic, colorectal, and lung cancers^[1].

IC₅₀ & Target

KRas G12C

0.457 μM (IC₅₀)

分子量

452.33

Formula

C₂₀H₁₆Cl₂FN₃O₂S

CAS 号

2230873-67-1

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]. Brian Alan LANMAN, et al. Kras g12c inhibitors and methods of using the same. US20180334454A1.

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标签归档：kras

MRTX-EX185

MRTX1133 formic

ASP2453

PROTAC KRAS G12C degrader-1

KRA-533

KRAS G13D peptide, 25 mer

KRAS G13D peptide, 25 mer

KRAS G13D peptide, 25 mer

SAH-SOS1A

SAH-SOS1A

SAH-SOS1A

KRAS G12D inhibitor 15

KRAS G12D inhibitor 6

KRAS G12D inhibitor 7

KRAS G12D inhibitor 6

KRAS G12D inhibitor 7

KRAS G12D inhibitor 6

KRAS G12D inhibitor 7

KRAS inhibitor-14

KRAS inhibitor-16