RET-IN-4


Catalog No. Size PriceQuantity
M17364-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

RET-IN-4 is a potent, selective and orally active RET inhibitor with IC50s of 1.29 nM, 1.97 nM, and 0.99 nM for RET (WT), RET (V804M), and RET (M918T), respectively. RET-IN-4 exhibits better kinases selectivity against JAK2 (IC50 of 4.4 nM) and FLT3 (IC50 of 30.8 nM). RET-IN-4 has anticancer effects.

Product information

CAS Number: 2436473-55-9

Molecular Weight: 546.60

Formula: C27H31FN10O2

Chemical Name: 4-[(1S)-1-[6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethyl]-9-{4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl}-1-oxa-4,9-diazaspiro[5.5]undecan-5-one

Smiles: CC1C=C(NC2C=C(C)NN=2)N=C(N=1)N1CCC2(CC1)OCCN([C@@H](C)C1=CN=C(C=C1)N1C=C(F)C=N1)C2=O

InChiKey: DIMALNWQSQDLJJ-IBGZPJMESA-N

InChi: InChI=1S/C27H31FN10O2/c1-17-12-22(32-23-13-18(2)34-35-23)33-26(31-17)36-8-6-27(7-9-36)25(39)37(10-11-40-27)19(3)20-4-5-24(29-14-20)38-16-21(28)15-30-38/h4-5,12-16,19H,6-11H2,1-3H3,(H2,31,32,33,34,35)/t19-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

The proliferation of Ba/F3 cells transformed with NSCLC related KIF5B-RET fusion is effectively suppressed by RET-IN-4 (compound 9) (IC50 of 19 nM). RET-IN-4 displays less ‘off-target’ effects than BLU-667.

In Vivo:

RET-IN-4 (compound 9; p.o.; 10-20 mg/kg; p.o.; daily; for 10 days) treatment represses tumor growth driven by KIF5B-RET-Ba/F3 cells in a dose-dependent manner.

Products are for research use only. Not for human use.

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