- SHP099
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- $31.00
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2026-07-27
- CAS:1801747-42-1
- Purity: 99.48%
- Supply Ability: 10g
- SHP099
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- $3.49
-
2022-02-25
- CAS:1801747-42-1
- Min. Order: 1KG
- Purity: 98%
- Supply Ability: 10kg
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| Product Name: | SHP099 | | Synonyms: | 6-(4-Amino-4-methyl-1-piperidinyl)-3-(2,3-dichlorophenyl)-2-pyrazinamine;6-(4-Azanyl-4-Methyl-Piperidin-1-Yl)-3-[2,3-Bis(Chloranyl)phenyl]pyrazin-2-Amine;SHP099;6-(4-amino-4-methylpiperidin-1-yl)-3-(2,3-dichlorophenyl)pyrazin-2-amine;SHP-099 (free base);2-Pyrazinamine, 6-(4-amino-4-methyl-1-piperidinyl)-3-(2,3-dichlorophenyl)-;SHP099, 10 mM in DMSO;SHP-099 (SHP099) | | CAS: | 1801747-42-1 | | MF: | C16H19Cl2N5 | | MW: | 352.26 | | EINECS: | | | Product Categories: | | | Mol File: | 1801747-42-1.mol |  |
| | SHP099 Chemical Properties |
| Boiling point | 530.4±50.0 °C(Predicted) | | density | 1.326±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Water:1.0(Max Conc. mg/mL);2.84(Max Conc. mM)
DMSO:21.0(Max Conc. mg/mL);34.07(Max Conc. mM) | | form | A crystalline solid | | pka | 9.05±0.20(Predicted) | | color | Light yellow to yellow | | InChI | InChI=1S/C16H19Cl2N5/c1-16(20)5-7-23(8-6-16)12-9-21-14(15(19)22-12)10-3-2-4-11(17)13(10)18/h2-4,9H,5-8,20H2,1H3,(H2,19,22) | | InChIKey | YGUFCDOEKKVKJK-UHFFFAOYSA-N | | SMILES | C1(N)=NC(N2CCC(N)(C)CC2)=CN=C1C1=CC=CC(Cl)=C1Cl |
| | SHP099 Usage And Synthesis |
| Uses | SHP099 is an allosteric SHP2 inhibitor, with IC50s of 0.690, 1.241, 0.416, 1.968, 2.896 μM for SHP2, SHP2D61Y, SHP2E69K, SHP2A72V, SHP2E76K. SHP099 inhibits cancer cell growth, such as MV4-11 and TF-1 cell (IC50: 0.32 and 1.73 μM). SHP099 inhibits RAS-ERK signaling and inhibits tumor growth[1][2]. | | in vivo | After a single dose of 30 and 100 mg/kg (red and blue lines, respectively), dose-dependent exposure and modulation of the pharmacodynamic marker p-ERK is observed in the xenografts. A daily oral dose of 10 or 30 mg/kg yield 19% and 61% tumor growth inhibition, respectively. Tumor stasis is achieved at 100 mg/kg[1]. | | References | [1] Chen YN, et al. Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases. Nature. 2016 Jul 7;535(7610):148-52. DOI:10.1038/nature18621
[2] Sun X, et al. Selective inhibition of leukemia-associated SHP2E69K mutant by the allosteric SHP2 inhibitor SHP099. Leukemia. 2018 May;32(5):1246-1249. DOI:10.1038/s41375-018-0020-5 |
| | SHP099 Preparation Products And Raw materials |
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