4,6-Dichloroisatin

Names

[ Name ]:
4,6-Dichloroisatin

[Synonym ]:
4,6-dichloro-2,3-dihydro-1H-indole-2,3-dione
1H-indole-2,3-dione, 4,6-dichloro-
4,6-dichloroisatine
4,6-DICHLORO-1H-INDOLE-2,3-DIONE
4,6-dichloroindolin-2,3-dione
4,6-Dichlor-indolin-2,3-dion
4,6-dichloroisatin
4,6-dichloro-indoline-2,3-dione

Biological Activity

[Description]:

CFL-120 is a potent KRasG12C inhibitor. CFL-120 shows an antiproliferative effect. CFL-120 shows anticancer activity. CFL-120 has the potential for the research of lung cancer[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> Ras

[Target]

KRAS(G12C)

[In Vitro]

CFL-120 (72 h) 显示出抗增殖作用，对 H1792, SW1573, MiaPaca2, H358, A549, SW480, PANC-1, LCLC-103H, BxPC3, HCA-7, MRC-5, HUVEC-TERT, CCD-986Sk 细胞的 IC50 值分别为 111.0, 23.6, 13.7, 16.9, 44.4, 14.8, 38.0, 30.0, 13.1, 9.8, 47.9, 24.4, 42.7 µM[1]。

[In Vivo]

CFL-120 (5 mg/kg，5 次治疗；15 mg/kg，5 次治疗；30 mg/kg，3 次治疗；i.p.) 减少皮下人肺癌 H1792 (KRasG12C 突变体) 和 LCLC-103H (KRasWT) 小鼠肿瘤模型的生长[1]。 Animal Model: NOD/SCID female mice (KRasWT (LCLC-103H) or KRasG12C (H1792) tumors)[1] Dosage: 5 mg/kg, 5 treatments; 15 mg/kg, 5 treatments; 30 mg/kg, 3 treatments Administration: I.p. Result: Reduced tumor growth compared to the control group in KRasG12C mutated model for 35.8%.

[References]

[1]. Orgován Z, et al. Covalent fragment mapping of KRasG12C revealed novel chemotypes with in vivo potency. Eur J Med Chem. 2023 Mar 15;250:115212.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Melting Point ]:
260.5-261°C

[ Molecular Formula ]:
C₈H₃Cl₂NO₂

[ Molecular Weight ]:
216.02

[ Exact Mass ]:
214.954086

[ PSA ]:
46.17000

[ LogP ]:
2.20

[ Index of Refraction ]:
1.638

Safety Information

[ Hazard Codes ]:
T+

[ RIDADR ]:
2811.0

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%