2843690-50-4
Chemical Structure
I-0436650
- CAS No.: 2843690-50-4
- Formula:C22H22ClN9S
- Molecular Weight:479.99
InChIKey: VUJLHBJEBKDVNJ-HXUWFJFHSA-N
SMILES: ClC1=C(N2C=CC=N2)N=CC=C1SC3=NC=C(N4CCC5(CC4)[C@@H](C6=CC=NN6C5)N)N=C3
Biological Activity: I-0436650 is an orally active SHP2 inhibitor with an IC50 of 4 nM and a Kd value of 0.3 nM. I-0436650 binds allosterically to the channel between the C-SH2, N-SH2 and PTP catalytic domains, locking the protein in an inactive closed conformation. I-0436650 potently inhibits ERK phosphorylation and suppresses MAPK pathway activity. I-0436650 exhibits antiproliferative activity in EGFR- and RAS-dependent cells. I-0436650 can be used in the research of RAS-driven cancers, EGFR-mutated cancers and RTK-driven cancers[1].
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I-0436650 | I-0436650 is an orally active SHP2 inhibitor with an IC50 of 4 nM and a Kd value of 0.3 nM. I-0436650 binds allosterically to the channel between the C-SH2, N-SH2 and PTP catalytic domains, locking the protein in an inactive closed conformation. I-0436650 potently inhibits ERK phosphorylation and suppresses MAPK pathway activity. I-0436650 exhibits antiproliferative activity in EGFR- and RAS-dependent cells. I-0436650 can be used in the research of RAS-driven cancers, EGFR-mutated cancers and RTK-driven cancers. | |||||||||||||||||||||
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