Cat. No.: HY-176954

RSC-1255

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RSC-1255 is a potent and selective Vacuolar H⁺-ATPase (V-ATPase) inhibitor that directly binds the mammalian V-ATPase complex with a K_d = 23 nM. RSC-1255 exhibits preferential cytotoxicity toward KRAS-mutant cancer cells, especially KRAS^G13D and KRAS^G12V cells. RSC-1255 induces apoptosis and blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers.

For research use only. We do not sell to patients.

Purity: 99.91%
CAS No.: 2171015-78-2
Formula: C₂₇H₂₅ClF₄N₄O₃
Molecular Weight:564.96

Storage:

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

RSC-1255 Chemical Structure

CAS No.: 2171015-78-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

KRAS G13D

KRas G12V

All Ras Isoforms :

In Vitro

RSC-1255 (249C) (1 μM; 1 h) inhibits V-ATPase–mediated proton pumping and lysosomal acidification in HEK293T cells^[1].
RSC-1255 (1 μM; 1 h) disrupts V-ATPase assembly by increasing membrane-associated V1 subunits in HEK293T cells^[1].
RSC-1255 exhibits potent growth-inhibitory activity in human cancer cell lines, with IC₅₀ values of 0.073 μM in A549 (KRAS-mutant), 0.06 μM in LOX IMVI (BRAFV600E), and 0.022μM in MelJuso (HRAS^G13D/NRAS^Q61L) cells^[1].
RSC-1255 (0-10 μM; 72 h) selectively reduces cell viability in KRAS-mutant mouse embryonic fibroblasts (MEFs) with the highest sensitivity in KRAS^G13D and KRAS^G12V cells^[1].
RSC-1255 (1 μM; 2-24 h) blocks autophagic flux, increasing SQSTM1/p62 and LC3-II accumulation in A549 cells^[1].
RSC-1255 (1 μM; 1 h) increases lysosomal pH in KRAS^G13D MEFs, reversing their highly acidic basal lysosomal state^[1].
RSC-1255 (1 μM; 1 h) inhibits V-ATPase–dependent proton transport in FITC-loaded lysosomes, showing the strongest inhibition in KRAS^G13D MEFs^[1].
RSC-1255 (1 μM; 24 h) enlarges autophagic vesicles and blocks lysosome-autophagosome fusion in KRAS^G13D, KRAS^G12V and BRAF^V600E MEFs^[1].
RSC-1255 (1 μM; 2 h) markedly reduces macropinocytosis levels in MEFs, with KRAS^G13D cells showing the strongest suppression^[1].
RSC-1255 ((1 μM; 24 h) induces apoptosis in KRAS-mutant MEFs, with KRAS^G13D, KRAS^G12V and BRAF^V600E cells showing the highest Annexin V^⁺/PI^⁺levels^[1].

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

Western Blot Analysis^[1]

Cell Line:

HEK293T cells
Concentration:

1 μM
Incubation Time:

1h
Result:

Increased membrane-associated V1 subunit B2 was observed, indicating altered V-ATPase assembly after treatment.

Western Blot Analysis^[1]

Cell Line:

A549 cells
Concentration:

1 μM
Incubation Time:

2 , 4 , 8 , 20 , 24 h
Result:

Time-dependent accumulation of SQSTM1/p62 and LC3-II, indicating autophagic flux inhibition.

Cell Viability Assay^[1]

Cell Line:

MEF KRAS mutants (KRAS^G13D, KRAS^G12V, KRAS^G12D, KRAS^G12S, KRAS^G12C, KRAS^Q61L, KRAS^Q61R, WT)
Concentration:

0-10 μM
Incubation Time:

72 h
Result:

Highest sensitivity in KRAS^G13D and KRAS^G12V MEFs with the lowest IC₅₀ values; minimal sensitivity in WT MEFs.

Apoptosis Analysis^[1]

Cell Line:

MEFs expressing KRAS^G13D, KRAS^G12V, BRAF^V600E and other KRAS mutants
Concentration:

1 μM
Incubation Time:

24h
Result:

Increased of Annexin V⁺/PI⁺ apoptotic cells, with KRAS^G13D,KRAS^G12V and BRAF^V600E MEFs showing the strongest apoptotic responses.

In Vivo

RSC-1255 (249C) (10 mg/kg; intraperitoneal (i.p.) injection; once or twice daily) significantly inhibits tumor growth in KRAS-mutant lung cancer and KRAS-mutant colorectal cancer xenograft models in mice^[1].

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

Animal Model:

A549 (KRAS^G12S) lung cancer xenografts were established in five-week-old athymic mice.
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection (i.p.); twice daily
Result:

Significantly reduced tumor volumes in A549 xenograft-bearing mice during the treatment period.
Increased LC3-I/II levels in tumor tissues, indicating autophagy inhibition in vivo.
No significant systemic toxicity, with normal body weight, organ weights and hematological parameters.

Animal Model:

SW48 xenograft models bearing parental or KRAS-mutant SW48 cells (KRAS^G12D/+, KRAS^G12V/+, KRAS^G13D/+) were established in five-six-week-old athymic mice].
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection (i.p.); 2 weeks.
Result:

Significant tumor growth inhibition in KRAS-mutant SW48 xenografts, with the strongest effects in KRAS^G13D/+ and KRAS^G12V+ tumors.
Minimal response in parental SW48 tumors, consistent with lower in vitro sensitivity.
No significant changes in body weight or systemic toxicity during treatment.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2171015-78-2
Appearance Solid
Molecular Weight 564.96
Formula C₂₇H₂₅ClF₄N₄O₃
Color Off-white to light yellow
SMILES

O=C(C1(C)N(C2=CC=C(C=C2F)F)N=C(C1C3=CC=C(Cl)O3)C4=C(F)C=C(F)C=C4)NCC5OCCN(C5)C
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 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]. Tolani B, et al. Ras-mutant cancers are sensitive to small molecule inhibition of V-type ATPases in mice. Nat Biotechnol. 2022;40(12):1834-1844. [Content Brief]

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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.

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RSC-1255

Apoptosis Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Membrane Transporter/Ion Channel Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

KRAS Targeted Compound Library

All Ras Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

RSC-1255 Related Classifications

HY-176954 Related Classifications