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Cat. No.: HY-175025

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CH091138

CH091138 is a potent and selective KRASG12D PROTAC degrader with DC₅₀s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS^WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)).
(Pink: KRas G12D ligand (HY-175144); Blue: VHL ligand (HY-138678); Black: linker).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₅₉H₆₉FN₁₀O₆S
분자량:1065.31

보관:

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

Data Sheet (274 KB)

CH091138 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

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

Biological Activity

제품 설명

CH091138 is a potent and selective KRASG12D PROTAC degrader with DC₅₀s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS^WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B))^[1]. (Pink: KRas G12D ligand (HY-175144); Blue: VHL ligand (HY-138678); Black: linker).

IC₅₀ & Target^[1]

KRas G12C

KRas G12D

KRas G12V

NEP108

3.8 μM (DC₅₀)

VHL

All PROTACs Isoforms :

All Ras Isoforms :

In Vitro

CH091138 (0-30 μM, 24 h) blocks KRAS downstream signaling in cells harboring KRAS^G12D in AsPC1 cells^[1].
CH091138 (0.01-100 μM, 3 days) exhibits a GI₅₀ of 0.75 μM in KRAS^G12D mutant AsPC1 cells^[1].
CH091138 (1-30 μM, 24 h) suppresses migration and invasion of AsPC-1^[1].
CH091138 (1-10 μM, 24 h-21 d) is capable of suppressing colony formation and induces apoptosis of AsPC-1^[1].
CH091138 (0-100 μM, 5 days) suppresses the growth of patient-derived organoids (PDOs) harboring KRAS^G12D more strongly than those with wild-type KRAS^[1].

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

Western Blot Analysis^[1]

Cell Line:

AsPC1-cells
Concentration:

0, 10, 30 μM
Incubation Time:

24 h
Result:

Effectively inhibited KRAS-dependent downstream pathways p-AKT, p-MEK and p-ERK1/2 levels.
Had no effect on other KRAS mutant cells.

Cell Viability Assay^[1]

Cell Line:

Human-derived organoids (PDOs) with wild-type KRAS (COL-032-T and COL-047-T) and KRAS^G12D mutation (COL-018-T and COL-049-T)
Concentration:

0, 16.7 and 50 μM
Incubation Time:

5 days
Result:

Exhibited an IC₅₀ of 12.62-33.13 μM for KRAS^G12D PDO.
Exhibited an IC₅₀ > 50 μM for KRAS^WT PDO.

In Vivo

CH091138 (60 mg/kg , i.p., once every three days for 29 days) has a remarkable in vivo anti-tumoral activity with little weight change in the AsPC-1 xenograft model^[1].

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

Animal Model:

Xenograft model bearing AsPC-1 cells established in five-week-old female Balb/C nude mice^[1]
Dosage:

60 mg/kg
Administration:

Intraperitoneal injection (i.p.) once every three days for 29 days
Result:

Achieved 61.8 % tumor growth inhibition.
Significantly decreased the average tumor weight and size.
Caused a decrease in KRAS level by up to 76.04 %.

Chemical Information

분자량 1065.31
화학식 C₅₉H₆₉FN₁₀O₆S
SMILES

OC1=CC(C=CC=C2C#C)=C2C(C3=C(F)C(N=C(OC[C@@H]4CCCN4CCCCCCC(N[C@H](C(N5[C@H](C(NCC6=CC=C(C7=C(C)N=CS7)C=C6)=O)C[C@@H](O)C5)=O)C(C)(C)C)=O)N=C8N9C[C@H]%10N[C@H](CC%10)C9)=C8C=N3)=C1
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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]. Jeon E,et al. KRASG12D selective VHL-PROTAC with sparing KRASWT and other KRAS mutants. Eur J Med Chem. 2025 Jul 5;297:117928. [Content Brief]

Calculators

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)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
CAS No.:
Species:
Purity:
수량:

CH091138

All PROTACs Isoforms

All Ras Isoforms