2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]-
- CAS No.
- 2417987-45-0
- Chemical Name:
- 2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]-
- Synonyms
- GDC-6036;divarasib;GDC6036 ,E1187;GDC-6036(Divarasib);Divarasib (GDC-6036);1-((S)-4-(7-((R)-6-Amino-4-methyl-3-(trifluoromethyl)pyridin-2-yl)-6-chloro-8-fluoro-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)quinazolin-4-yl)-3-methylpiperazin-1-yl)prop-2-en-1-one;2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]-
- CBNumber:
- CB010801323
- Molecular Formula:
- C29H32ClF4N7O2
- Molecular Weight:
- 622.06
- MDL Number:
- MOL File:
- 2417987-45-0.mol
- MSDS File:
- SDS
| Product description | Number | Pack Size | Price |
| GDC-6036 ≥98% | 41852 | 500μg | $109 |
| GDC-6036 ≥98% | 41852 | 1mg | $207 |
| GDC-6036 ≥98% | 41852 | 5mg | $763 |
| GDC-6036 ≥98% | 41852 | 10mg | $1089 |
| Divarasib 99.31% | CS-0435408 | 1mg | $325 |
2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]- Properties
| Boiling point | 743.4±70.0 °C(Predicted) |
|---|---|
| Density | 1.344±0.06 g/cm3(Predicted) |
| storage temp. | Store at -20°C |
| solubility |
DMSO: Soluble: =10 mg/ml Ethanol: Slightly soluble: 0.1-1 mg/ml |
| form | Solid |
| pka | 9.13±0.40(Predicted) |
| color | White to light yellow |
| FDA UNII | E6S21PVT91 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) | ![]() GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319 |
| Precautionary statements | P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330 |
2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]- price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 41852 | GDC-6036 ≥98% | 2417987-45-0 | 500μg | $109 | 2026-04-30 | Buy |
| Cayman Chemical | 41852 | GDC-6036 ≥98% | 2417987-45-0 | 1mg | $207 | 2026-04-30 | Buy |
| Cayman Chemical | 41852 | GDC-6036 ≥98% | 2417987-45-0 | 5mg | $763 | 2026-04-30 | Buy |
| Cayman Chemical | 41852 | GDC-6036 ≥98% | 2417987-45-0 | 10mg | $1089 | 2026-04-30 | Buy |
| ChemScene | CS-0435408 | Divarasib 99.31% | 2417987-45-0 | 1mg | $325 | 2026-06-04 | Buy |
2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]- Chemical Properties,Uses,Production
Uses
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
in vivo
Divarasib (10-100 mg/kg/day; PO for 7 days) decreases the ratio of free KRAS G12C[1].
| Animal Model: | Female C.B-17 SCID (Inbred) mice (20-21 weeks old; 24.1 g) with human NSCLC NCI-H2030.X1.1 cells[1] |
| Dosage: | 10, 25, or 100 mg/kg |
| Administration: | Oral gavage (PO) every day (QD) for 7 days (vehicle: 0.5% methylcellulose) |
| Result: | Decreased the ratio of free KRAS G12C to internal standard. Dose-dependent target engagement was observed for all time points (2, 8, and 24 h post-last dose), with over 90% KRAS G12C engagement observed for the highest dose 100 mg/kg assessed. |
IC 50
K-Ras(G12C): <0.01 μM (IC50)
References
[1] Lingyao Meng, et al. Assessment of KRAS G12C Target Engagement by a Covalent Inhibitor in Tumor Biopsies Using an Ultra-Sensitive Immunoaffinity 2D-LC-MS/MS Approach. Anal Chem. 2022 Sep 20;94(37):12927-12933. DOI:10.1021/acs.analchem.2c03146
[2] Sushant Malhotra, et al. Fused ring compounds. WO2020097537A2.
[3] JOHN C. TRAN*, MARK MERCHANT* Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry[J]. Analytical Chemistry, 2023, 95 11: 4834-4839. DOI: 10.1021/acs.analchem.2c04417
2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
2-Propen-1-one, 1-[(3S)-4-[(7R)-7-[6-amino-4-methyl-3-(trifluoromethyl)-2-pyridinyl]-6-chloro-8-fluoro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]-4-quinazolinyl]-3-methyl-1-piperazinyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Nantong HI-FUTURE Biology Co., Ltd. | +86-18051384581 | sales@chemhifuture.com | China | 3135 | 58 |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 33024 | 60 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 | marketing@targetmol.com | United States | 32468 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 | sales@sarms4muscle.com | China | 10457 | 58 |
| Zibo Hangyu Biotechnology Development Co., Ltd | +86-0533-2185556 +86-15965530500 | nickzhang@hangyubiotech.com | China | 9941 | 58 |
| Suzhou ARTK Medchem Co., Ltd. | +86-18168183658 | sales1@artkmedchem.com | China | 39021 | 58 |
| NANJING YINGWEN BIOTECHNOLOGY CO LTD | +86-13382787392 | sales@aeechem.com | China | 10002 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3504 | 58 |
| Chunchuang (Wuhan) Technology Co., Ltd | 15727060112 | yutianchun2007@126.com | China | 9863 | 58 |
| Chengdu DingDang Pharmaceutical Co., Ltd. | 028-86040038 | market@dingdangchem.com | China | 1854 | 55 |






