ChemicalBook > CAS DataBase List > Amgen IRE1α Inhibitor

Amgen IRE1α Inhibitor

Product Name: Amgen IRE1α Inhibitor
CAS No.: 1630086-20-2
Chemical Name: Amgen IRE1α Inhibitor
Synonyms: Kira8;Kira8 ，E2652;KIRA8 (AMG-18);IRE-1 INHIBITOR;Kira8, 10 mM in DMSO;Amgen IRE1± Inhibitor;Amgen IRE1α Inhibitor;Amgen IRE1a Inhibitor;Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8;(S)-2-Chloro-N-[6-methyl-5-[[3-[2-(3-piperidylamino)-4-pyrimidinyl]-2-pyridyl]oxy]-1-naphthyl]benzenesulfonamide
CBNumber: CB73123772
Molecular Formula: C31H29ClN6O3S
Formula Weight: 601.12
MOL File: 1630086-20-2.mol

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Amgen IRE1α Inhibitor Property

Boiling point:: 812.6±75.0 °C(Predicted)
Density: 1.383±0.06 g/cm3(Predicted)
storage temp.: Store at -20°C
solubility: Water:30.0(Max Conc. mg/mL);49.91(Max Conc. mM)
form: Solid
pka: 7.66±0.30(Predicted)
color: Light yellow to yellow

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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: VBP00322
Product name: (S)-2-chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide
Purity: Aldrich<SUP>CPR</SUP>
Packaging: 10 mg
Price: $1420
Updated: 2025/07/31

TRC

Product number: A576530
Product name: AmgenIRE1αInhibitor
Packaging: 10mg
Price: $1320
Updated: 2021/12/16

ChemScene

Product number: CS-0084229
Product name: Kira8
Purity: 99.74%
Packaging: 5mg
Price: $320
Updated: 2021/12/16

ChemScene

Product number: CS-0084229
Product name: Kira8
Purity: 99.74%
Packaging: 10mg
Price: $520
Updated: 2021/12/16

Crysdot

Product number: CD11242815
Product name: (S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide
Purity: 97%
Packaging: 5mg
Price: $689
Updated: 2021/12/16

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Amgen IRE1α Inhibitor Chemical Properties,Usage,Production

Uses

Amgen IRE1α Inhibitor is an inhibitor of IRE1α. IRE1α is a sensor of unfolded protein accumulation that triggers the unfolded protein response.

Biological Activity

KIRA8 is an ATP-competitive, potent and selective IRE1α kinase inhibitor (IRE1α/β Ki = 2/120 nM) th at attenuates IRE1α endonuclease activity (IRE1α/β IC50 = 5/55 nM) with good kinome selectivity. KIRA8 inhibits thapsigargin-induced UPR (IC50 = 99 nM; HT1080 XBP1-Luc cells) and shows therapeutic efficacy in murine models of type 1 diabetes (T1D), pulmonary fibrosis, multiple myeloma (MM), and pancreatic neuroendocrine tumors (PanNET) in vivo (30-50 mg/kg/day i.p.).

in vivo

Male Ins2^+/Akita mice are injected i.p. with KIRA8 (50 mg/kg; daily; for 35 days), significant reduction of hyperglycemia become apparent over several weeks^[1].
? One week treatment of pre-diabetic NODs mice with Kira8 (50 mg/kg; i.p.; once a day) leads to significant reductions in islet XBP1 splicing and TXNIP mRNAs, and preserves Ins1/Ins2, BiP and MANF mRNAs^[1].

Animal Model:	Male Ins2^+/Akita mice^[1]
Dosage:	50 mg/kg
Administration:	Injected i.p.; daily; for 35 days
Result:	Significant reduction of hyperglycemia became apparent over several weeks.

Amgen IRE1α Inhibitor Preparation Products And Raw materials

Raw materials

Preparation Products

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1630086-20-2, Amgen IRE1α InhibitorRelated Search:

Kira8

Amgen IRE1α Inhibitor

IRE-1 INHIBITOR

KIRA8 (AMG-18)

Benzenesulfonamide, 2-chloro-N-[6-methyl-5-[[3-[2-[(3S)-3-piperidinylamino]-4-pyrimidinyl]-2-pyridinyl]oxy]-1-naphthalenyl]-

(S)-2-Chloro-N-(6-methyl-5-((3-(2-(piperidin-3-ylamino)pyrimidin-4-yl)pyridin-2-yl)oxy)naphthalen-1-yl)benzenesulfonamide

Amgen IRE1a Inhibitor

Inositol requiring enzyme 1,inhibit,AMG18,AMG 18,Kira 8,Kira8,Inhibitor,IRE1,Kira-8

(S)-2-Chloro-N-[6-methyl-5-[[3-[2-(3-piperidylamino)-4-pyrimidinyl]-2-pyridyl]oxy]-1-naphthyl]benzenesulfonamide

Kira8, 10 mM in DMSO

Amgen IRE1± Inhibitor

Kira8 ，E2652

1630086-20-2

C31H29ClN6O3S