Drug Information

Drug (ID: DG01643) and It's Reported Resistant Information

Name	FF-10101
Synonyms	FF-10101; 1472797-69-5; UNII-7V7IHI0SYG; 7V7IHI0SYG; (S,E)-N-(1-((5-(2-((4-Cyanophenyl)amino)-4-(propylamino)pyrimidin-5-yl)pent-4-yn-1-yl)amino)-1-oxopropan-2-yl)-4-(dimethylamino)-N-methylbut-2-enamide; CHEMBL4650283; SCHEMBL15584726; SCHEMBL16443760; BDBM397428; BCP23613; s8899; US9987278, Compound Reference 38; Ff-10101-01; HY-109584; CS-0032038; FF 10101; FF10101; D87147; (E)-N-[(2S)-1-[5-[2-(4-cyanoanilino)-4-(propylamino)pyrimidin-5-yl]pent-4-ynylamino]-1-oxopropan-2-yl]-4-(dimethylamino)-N-methylbut-2-enamide; 2-Butenamide, N-((1S)-2-((5-(2-((4-cyanophenyl)amino)-4-(propylamino)-5-pyrimidinyl)-4-pentyn-1-yl)amino)-1-methyl-2-oxoethyl)-4-(dimethylamino)-N-methyl-, (2E)- Click to Show/Hide
Indication	In total 1 Indication(s) Hepatitis C virus infection [ICD-11: 1E50-1E51] Phase 1/2 [1]
Structure
Target	Hepatitis C virus NS3 helicase (HCV NS3)	POLG_HCV1	[1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula	14
IsoSMILES	CCCNC1=NC(=NC=C1C#CCCCNC(=O)[C@H](C)N(C)C(=O)/C=C/CN(C)C)NC2=CC=C(C=C2)C#N
InChI	InChI=1S/C29H38N8O2/c1-6-17-31-27-24(21-33-29(35-27)34-25-15-13-23(20-30)14-16-25)11-8-7-9-18-32-28(39)22(2)37(5)26(38)12-10-19-36(3)4/h10,12-16,21-22H,6-7,9,17-19H2,1-5H3,(H,32,39)(H2,31,33,34,35)/b12-10+/t22-/m0/s1
InChIKey	HJFSVYUFOXAVAA-YUAYGMJFSA-N
PubChem CID	90052320
TTD Drug ID	D07TYE

Type(s) of Resistant Mechanism of This Drug

UAPP: Unusual Activation of Pro-survival Pathway

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-02: Benign/in-situ/malignant neoplasm

Click to Show/Hide the Resistance Disease of This Class

Hematologic cancer [ICD-11: 2B3Z]

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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
Unusual Activation of Pro-survival Pathway (UAPP)			Click to Show/Hide
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT)				[1]
Molecule Alteration	Missense mutation		p.D816V (c.2447A>T)	Molecule Info
Sensitive Disease	Hematologic Cancer [ICD-11: MG24.Y]			Disease Info
Experimental Note	Identified from the Human Clinical Data
In Vitro Model	HEK293T cells	Kidney	Homo sapiens (Human)	CVCL_0063
In Vivo Model	NOD/SCID mouse PDX model			Mus musculus
Experiment for Molecule Alteration	Western blotting analysis
Experiment for Drug Resistance	Colony formation assay

References

Ref 1	A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells with FLT3 mutationsBlood. 2018 Jan 25;131(4):426-438. doi: 10.1182/blood-2017-05-786657. Epub 2017 Nov 29.