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SB 202190 是選擇性的 p38 MAPK 抑制劑,抑制 p38α 和 p38β2 的 IC50 分別為 50 nM 和 100 nM。SB 202190 與重組人活性 p38 激酶的 ATP 袋結(jié)合,Kd 值為 38 nM。SB 202190 具有抗癌活性并可以挽救記憶障礙。
生物活性
SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits[1][2]. SB202190 induces autophagy[3]
體外研究(In Vitro)
SB 202190 (0-10 μM; 0-72 hours) attenuates growth of a subgroup of CRC cell lines such as RKO, CACO2 and SW480 in a dose- and time-dependent manner[1].
SB 202190 strongly inhibited colony formation and anchorage-independent growth (10 μM for 7–10 days) and elevated apoptotic cell death (10 μM for 72 h) in this same subset of CRC lines (RKO, CACO2 and SW480)[2].
In RKO, CACO2 and SW480 cells, SB202190 (10 μM; 2 hours) abrogates phosphorylation of S6K1(T389) and S6(S235/236), but not AKT(S473), indicating that p38i selectively blocks mTORC1 signaling
體內(nèi)研究(In Vivo)
SB 202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) shows inhibition of tumor cell survival and tumor growth[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | 4-week-old female BALB/c nude mice (bearing SW480 and RKO xenograft tumors)[2] |
Dosage: | 5 mg/kg |
Administration: | Intraperitoneal injection; daily for 10-12 days |
Result: | Inhibition of tumor cell survival and tumor growth. |
分子量:331.34
Formula:C20H14FN3O
CAS 號(hào):152121-30-7
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (301.80 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.0180 mL | 15.0902 mL | 30.1805 mL |
5 mM | 0.6036 mL | 3.0180 mL | 6.0361 mL |
10 mM | 0.3018 mL | 1.5090 mL | 3.0180 mL |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
請(qǐng)依序添加每種溶劑: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.28 mM); Clear solution
參考文獻(xiàn)
SB 202190 是選擇性的 p38 MAPK 抑制劑,抑制 p38α 和 p38β2 的 IC50 分別為 50 nM 和 100 nM。SB 202190 與重組人活性 p38 激酶的 ATP 袋結(jié)合,Kd 值為 38 nM。SB 202190 具有抗癌活性并可以挽救記憶障礙。
生物活性
SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits[1][2]. SB202190 induces autophagy[3]
體外研究(In Vitro)
SB 202190 (0-10 μM; 0-72 hours) attenuates growth of a subgroup of CRC cell lines such as RKO, CACO2 and SW480 in a dose- and time-dependent manner[1].
SB 202190 strongly inhibited colony formation and anchorage-independent growth (10 μM for 7–10 days) and elevated apoptotic cell death (10 μM for 72 h) in this same subset of CRC lines (RKO, CACO2 and SW480)[2].
In RKO, CACO2 and SW480 cells, SB202190 (10 μM; 2 hours) abrogates phosphorylation of S6K1(T389) and S6(S235/236), but not AKT(S473), indicating that p38i selectively blocks mTORC1 signaling
體內(nèi)研究(In Vivo)
SB 202190 (5 mg/kg; intraperitoneal injection; daily for 10-12 days) shows inhibition of tumor cell survival and tumor growth[2].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: | 4-week-old female BALB/c nude mice (bearing SW480 and RKO xenograft tumors)[2] |
Dosage: | 5 mg/kg |
Administration: | Intraperitoneal injection; daily for 10-12 days |
Result: | Inhibition of tumor cell survival and tumor growth. |
分子量:331.34
Formula:C20H14FN3O
CAS 號(hào):152121-30-7
運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式:
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
溶解性數(shù)據(jù)
DMSO : 100 mg/mL (301.80 mM; Need ultrasonic)
濃度溶劑體積質(zhì)量 | 1 mg | 5 mg | 10 mg |
---|
1 mM | 3.0180 mL | 15.0902 mL | 30.1805 mL |
5 mM | 0.6036 mL | 3.0180 mL | 6.0361 mL |
10 mM | 0.3018 mL | 1.5090 mL | 3.0180 mL |
請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用; 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶
請(qǐng)依序添加每種溶劑: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (6.28 mM); Clear solution
參考文獻(xiàn)