Cat. No.: HY-155356

YN14

Name: YN14
Brand: MedChemExpress
SKU: HY-155356
Price: 990.00 USD
Availability: InStock
Rating: 5 (1 reviews)

고객리뷰

Based on 1 Customer Validation

YN14 is a KRAS^G12C PROTAC degrader that recruits E3 ubiquitin ligase to induce the polyubiquitination and proteasomal degradation of KRAS^G12C. YN14 induces tumor cell apoptosis, cell cycle arrest, and cell migration inhibition. YN14 exhibits in vivo antitumor proliferative activity in tumor cell xenograft nude mice. YN14 can be used in cancer-related research.
(Pink: KRAS(G12C) ligand (HY-114277); Blue: VHL ligand (HY-125845); Black: linker (HY-W588704)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

Purity : 99.08%
화학식: C₆₂H₇₅F₂N₁₁O₇S
분자량:1156.39

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

YN14 Chemical Structure

사이즈

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재고

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
용액&용해도
- In Vitro
순도&문서
References
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

YN14 is a KRAS^G12C PROTAC degrader that recruits E3 ubiquitin ligase to induce the polyubiquitination and proteasomal degradation of KRAS^G12C. YN14 induces tumor cell apoptosis, cell cycle arrest, and cell migration inhibition. YN14 exhibits in vivo antitumor proliferative activity in tumor cell xenograft nude mice. YN14 can be used in cancer-related research^[1]. (Pink: KRAS(G12C) ligand (HY-114277); Blue: VHL ligand (HY-125845); Black: linker (HY-W588704)).

IC₅₀ & Target

^[1]

KRas G12C

Caspase 3

Akt

All PROTACs Isoforms :

All Ras Isoforms :

All Akt Isoforms :

All Caspase Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
ASPC1	IC₅₀	>10 μM Compound: YN14	Antiproliferative activity against human ASPC1 cells expressing KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human ASPC1 cells expressing KRAS G12D mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
HEK-293T	IC₅₀	>10 μM Compound: YN14	Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Cytotoxicity against HEK293T cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
HepG2	IC₅₀	>10 μM Compound: YN14	Antiproliferative activity against human HepG2 cells expressing KRAS assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HepG2 cells expressing KRAS assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
MIA PaCa-2	IC₅₀	0.045 μM Compound: YN14	Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MIA PaCa-2 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]
NCI-H358	IC₅₀	0.091 μM Compound: YN14	Antiproliferative activity against human NCI-H358 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H358 cells expressing KRAS G12C mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37852032]

In Vitro

YN14 (0-10000 nM; 72 h) effectively induces potent, concentration-dependent degradation of the KRAS^G12C protein in NCI-H358 non-small cell lung cancer cells and Miapaca-2 pancreatic cancer cells; its DC₅₀ is 0.067 μM in NCI-H358 and 0.028 μM in Miapaca-2^[1].
YN14 (30-300 nM; 24-48 h) induces apoptosis in NCI-H358 non-small cell lung cancer cells and Miapaca-2 pancreatic cancer cells, and arrests the cell cycle of NCI-H358 and Miapaca-2 cells at the G2/M phase in a dose-dependent manner^[1].
YN14 (30-300 nM; 12 h) inhibits the migration capacity of NCI‑H358 cells in a dose-dependent manner, exhibiting a dose-dependent effect^[1].

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

Western Blot Analysis^[1]

Cell Line:

NCI-H358 non-small cell lung cancer cells, Miapaca-2 pancreatic cancer cells
Concentration:

0 nM, 1 nM, 3.3 nM, 10 nM, 33 nM, 100 nM, 300 nM, 1000 nM, 3000 nM, 10000 nM
Incubation Time:

72 h
Result:

Induced concentration-dependent degradation of KRASG12C protein in NCI-H358 cells, with KRASG12C protein signal beginning to decrease markedly at 33 nM, partial residual KRASG12C signal remaining at 1000 nM, and full restoration of the KRASG12C signal at 10000 nM.
Induced gradual concentration-dependent reduction of KRASG12C protein levels in Miapaca-2 cells, with distinct KRASG12C protein degradation starting from 10 nM, and near-maximal KRASG12C degradation achieved at 100 nM and 300 nM.
Showed no alteration in β-actin signal intensity across all tested concentrations, confirming equal protein loading across all samples.

Cell Migration Assay ^[1]

Cell Line:

NCI-H358 non-small cell lung cancer cells
Concentration:

30, 100, 300 nM
Incubation Time:

12 h
Result:

Inhibited the migration capacity of NCI‑H358 cells in a dose-dependent manner, exhibiting a dose-dependent effect.

In Vivo

YN14 (10‑30 mg/kg; once daily, administered intraperitoneally; for 0-16 days) inhibits tumor growth in the BALB/c nude mouse xenograft model inoculated with human pancreatic cancer Miapaca‑2 cells, downregulates the protein levels of KRAS^G12C, CD31, p‑ERK, and p‑AKT in xenograft tumor tissues, and upregulates the protein level of the pro‑apoptotic marker cleaved‑caspase 3^[1].

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

Animal Model:

BALB/c nude mice (female, 4~6 weeks) were subcutaneously inoculated with 5×10⁶ Miapaca‑2 human pancreatic cancer cells.^[1]
Dosage:

10, 30 mg/kg
Administration:

Intraperitoneal (IP) injection; once daily; for 2, 4, 6, 8, 10, 12, 14, 16 days
Result:

Markedly suppressed tumour growth with TGI of 93.42 % measured on day 8 in the 10 mg/kg group, and no obvious body‑weight loss or toxic responses were observed in experimental animals.
Achieved TGI > 100 % measured on day 8 in the 30 mg/kg group, indicating tumour regression.
Revealed downregulation of KRAS^G12C, CD31, p‑ERK and p‑AKT, and upregulation of pro‑apoptotic marker cleaved‑caspase 3 in tumour tissues via immunohistochemistry and western‑blot assays.

Related Protocols :

Chemical Information

Appearance Solid
분자량 1156.39
화학식 C₆₂H₇₅F₂N₁₁O₇S
Color White to off-white
SMILES

O=C(C=C)N1C[C@H](C)N(C2=NC(N(C3=C(C)C=CN=C3C(C)C)C4=NC(C5=C(OCC6CCN(CCCC(N[C@@H](C(C)(C)C)C(N7[C@H](C(NCC8=CC=C(C9=C(C)N=CS9)C=C8)=O)C[C@@H](O)C7)=O)=O)CC6)C=CC=C5F)=C(F)C=C42)=O)CC1
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

용액&용해도

In Vitro:

DMSO : 100 mg/mL (86.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.8648 mL

4.3238 mL

8.6476 mL

5 mM

0.1730 mL

0.8648 mL

1.7295 mL

10 mM

0.0865 mL

0.4324 mL

0.8648 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Yang N, et al. Discovery of highly potent and selective KRASG12C degraders by VHL-recruiting PROTACs for the treatment of tumors with KRASG12C-Mutation. Eur J Med Chem. 2023 Dec 5;261:115857. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.8648 mL	4.3238 mL	8.6476 mL	21.6190 mL
	5 mM	0.1730 mL	0.8648 mL	1.7295 mL	4.3238 mL
	10 mM	0.0865 mL	0.4324 mL	0.8648 mL	2.1619 mL
	15 mM	0.0577 mL	0.2883 mL	0.5765 mL	1.4413 mL
	20 mM	0.0432 mL	0.2162 mL	0.4324 mL	1.0810 mL
	25 mM	0.0346 mL	0.1730 mL	0.3459 mL	0.8648 mL
	30 mM	0.0288 mL	0.1441 mL	0.2883 mL	0.7206 mL
	40 mM	0.0216 mL	0.1081 mL	0.2162 mL	0.5405 mL
	50 mM	0.0173 mL	0.0865 mL	0.1730 mL	0.4324 mL
	60 mM	0.0144 mL	0.0721 mL	0.1441 mL	0.3603 mL
	80 mM	0.0108 mL	0.0540 mL	0.1081 mL	0.2702 mL

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YN14

All PROTACs Isoforms

All Ras Isoforms

All Akt Isoforms

All Caspase Isoforms